An serine-threonine protein kinase that requires the presence of physiological concentrations of CALCIUM and membrane PHOSPHOLIPIDS. The additional presence of DIACYLGLYCEROLS markedly increases its sensitivity to both calcium and phospholipids. The sensitivity of the enzyme can also be increased by PHORBOL ESTERS and it is believed that protein kinase C is the receptor protein of tumor-promoting phorbol esters.
A family of enzymes that catalyze the conversion of ATP and a protein to ADP and a phosphoprotein.
A group of enzymes that are dependent on CYCLIC AMP and catalyze the phosphorylation of SERINE or THREONINE residues on proteins. Included under this category are two cyclic-AMP-dependent protein kinase subtypes, each of which is defined by its subunit composition.
A CALMODULIN-dependent enzyme that catalyzes the phosphorylation of proteins. This enzyme is also sometimes dependent on CALCIUM. A wide range of proteins can act as acceptor, including VIMENTIN; SYNAPSINS; GLYCOGEN SYNTHASE; MYOSIN LIGHT CHAINS; and the MICROTUBULE-ASSOCIATED PROTEINS. (From Enzyme Nomenclature, 1992, p277)
A group of enzymes that catalyzes the phosphorylation of serine or threonine residues in proteins, with ATP or other nucleotides as phosphate donors.
A superfamily of PROTEIN-SERINE-THREONINE KINASES that are activated by diverse stimuli via protein kinase cascades. They are the final components of the cascades, activated by phosphorylation by MITOGEN-ACTIVATED PROTEIN KINASE KINASES, which in turn are activated by mitogen-activated protein kinase kinase kinases (MAP KINASE KINASE KINASES).
Agents that inhibit PROTEIN KINASES.
The introduction of a phosphoryl group into a compound through the formation of an ester bond between the compound and a phosphorus moiety.
An intracellular signaling system involving the MAP kinase cascades (three-membered protein kinase cascades). Various upstream activators, which act in response to extracellular stimuli, trigger the cascades by activating the first member of a cascade, MAP KINASE KINASE KINASES; (MAPKKKs). Activated MAPKKKs phosphorylate MITOGEN-ACTIVATED PROTEIN KINASE KINASES which in turn phosphorylate the MITOGEN-ACTIVATED PROTEIN KINASES; (MAPKs). The MAPKs then act on various downstream targets to affect gene expression. In mammals, there are several distinct MAP kinase pathways including the ERK (extracellular signal-regulated kinase) pathway, the SAPK/JNK (stress-activated protein kinase/c-jun kinase) pathway, and the p38 kinase pathway. There is some sharing of components among the pathways depending on which stimulus originates activation of the cascade.
A mitogen-activated protein kinase subfamily that regulates a variety of cellular processes including CELL GROWTH PROCESSES; CELL DIFFERENTIATION; APOPTOSIS; and cellular responses to INFLAMMATION. The P38 MAP kinases are regulated by CYTOKINE RECEPTORS and can be activated in response to bacterial pathogens.
Phosphotransferases that catalyzes the conversion of 1-phosphatidylinositol to 1-phosphatidylinositol 3-phosphate. Many members of this enzyme class are involved in RECEPTOR MEDIATED SIGNAL TRANSDUCTION and regulation of vesicular transport with the cell. Phosphatidylinositol 3-Kinases have been classified both according to their substrate specificity and their mode of action within the cell.
A proline-directed serine/threonine protein kinase which mediates signal transduction from the cell surface to the nucleus. Activation of the enzyme by phosphorylation leads to its translocation into the nucleus where it acts upon specific transcription factors. p40 MAPK and p41 MAPK are isoforms.
Conversion of an inactive form of an enzyme to one possessing metabolic activity. It includes 1, activation by ions (activators); 2, activation by cofactors (coenzymes); and 3, conversion of an enzyme precursor (proenzyme or zymogen) to an active enzyme.
A cytoplasmic serine threonine kinase involved in regulating CELL DIFFERENTIATION and CELLULAR PROLIFERATION. Overexpression of this enzyme has been shown to promote PHOSPHORYLATION of BCL-2 PROTO-ONCOGENE PROTEINS and chemoresistance in human acute leukemia cells.
A serine-threonine protein kinase family whose members are components in protein kinase cascades activated by diverse stimuli. These MAPK kinases phosphorylate MITOGEN-ACTIVATED PROTEIN KINASES and are themselves phosphorylated by MAP KINASE KINASE KINASES. JNK kinases (also known as SAPK kinases) are a subfamily.
A ubiquitously expressed protein kinase that is involved in a variety of cellular SIGNAL PATHWAYS. Its activity is regulated by a variety of signaling protein tyrosine kinase.
A 44-kDa extracellular signal-regulated MAP kinase that may play a role the initiation and regulation of MEIOSIS; MITOSIS; and postmitotic functions in differentiated cells. It phosphorylates a number of TRANSCRIPTION FACTORS; and MICROTUBULE-ASSOCIATED PROTEINS.
A subgroup of mitogen-activated protein kinases that activate TRANSCRIPTION FACTOR AP-1 via the phosphorylation of C-JUN PROTEINS. They are components of intracellular signaling pathways that regulate CELL PROLIFERATION; APOPTOSIS; and CELL DIFFERENTIATION.
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
Intracellular signaling protein kinases that play a signaling role in the regulation of cellular energy metabolism. Their activity largely depends upon the concentration of cellular AMP which is increased under conditions of low energy or metabolic stress. AMP-activated protein kinases modify enzymes involved in LIPID METABOLISM, which in turn provide substrates needed to convert AMP into ATP.
A protein kinase C subtype that was originally characterized as a CALCIUM-independent, serine-threonine kinase that is activated by PHORBOL ESTERS and DIACYLGLYCEROLS. It is targeted to specific cellular compartments in response to extracellular signals that activate G-PROTEIN-COUPLED RECEPTORS; TYROSINE KINASE RECEPTORS; and intracellular protein tyrosine kinase.
PKC beta encodes two proteins (PKCB1 and PKCBII) generated by alternative splicing of C-terminal exons. It is widely distributed with wide-ranging roles in processes such as B-cell receptor regulation, oxidative stress-induced apoptosis, androgen receptor-dependent transcriptional regulation, insulin signaling, and endothelial cell proliferation.
Structurally related forms of an enzyme. Each isoenzyme has the same mechanism and classification, but differs in its chemical, physical, or immunological characteristics.
A PROTEIN-TYROSINE KINASE family that was originally identified by homology to the Rous sarcoma virus ONCOGENE PROTEIN PP60(V-SRC). They interact with a variety of cell-surface receptors and participate in intracellular signal transduction pathways. Oncogenic forms of src-family kinases can occur through altered regulation or expression of the endogenous protein and by virally encoded src (v-src) genes.
A phorbol ester found in CROTON OIL with very effective tumor promoting activity. It stimulates the synthesis of both DNA and RNA.
A group of cyclic GMP-dependent enzymes that catalyze the phosphorylation of SERINE or THREONINE residues of proteins.
Protein kinases that catalyze the PHOSPHORYLATION of TYROSINE residues in proteins with ATP or other nucleotides as phosphate donors.
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
Phosphoprotein with protein kinase activity that functions in the G2/M phase transition of the CELL CYCLE. It is the catalytic subunit of the MATURATION-PROMOTING FACTOR and complexes with both CYCLIN A and CYCLIN B in mammalian cells. The maximal activity of cyclin-dependent kinase 1 is achieved when it is fully dephosphorylated.
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH.
A ubiquitous casein kinase that is comprised of two distinct catalytic subunits and dimeric regulatory subunit. Casein kinase II has been shown to phosphorylate a large number of substrates, many of which are proteins involved in the regulation of gene expression.
Established cell cultures that have the potential to propagate indefinitely.
A multifunctional calcium-calmodulin-dependent protein kinase subtype that occurs as an oligomeric protein comprised of twelve subunits. It differs from other enzyme subtypes in that it lacks a phosphorylatable activation domain that can respond to CALCIUM-CALMODULIN-DEPENDENT PROTEIN KINASE KINASE.
The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.
Mitogen-activated protein kinase kinase kinases (MAPKKKs) are serine-threonine protein kinases that initiate protein kinase signaling cascades. They phosphorylate MITOGEN-ACTIVATED PROTEIN KINASE KINASES; (MAPKKs) which in turn phosphorylate MITOGEN-ACTIVATED PROTEIN KINASES; (MAPKs).
Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.
The rate dynamics in chemical or physical systems.
A dsRNA-activated cAMP-independent protein serine/threonine kinase that is induced by interferon. In the presence of dsRNA and ATP, the kinase autophosphorylates on several serine and threonine residues. The phosphorylated enzyme catalyzes the phosphorylation of the alpha subunit of EUKARYOTIC INITIATION FACTOR-2, leading to the inhibition of protein synthesis.
A family of serine-threonine kinases that bind to and are activated by MONOMERIC GTP-BINDING PROTEINS such as RAC GTP-BINDING PROTEINS and CDC42 GTP-BINDING PROTEIN. They are intracellular signaling kinases that play a role the regulation of cytoskeletal organization.
An abundant 43-kDa mitogen-activated protein kinase kinase subtype with specificity for MITOGEN-ACTIVATED PROTEIN KINASE 1 and MITOGEN-ACTIVATED PROTEIN KINASE 3.
A mitogen-activated protein kinase subfamily that is widely expressed and plays a role in regulation of MEIOSIS; MITOSIS; and post mitotic functions in differentiated cells. The extracellular signal regulated MAP kinases are regulated by a broad variety of CELL SURFACE RECEPTORS and can be activated by certain CARCINOGENS.
A family of protein serine/threonine kinases which act as intracellular signalling intermediates. Ribosomal protein S6 kinases are activated through phosphorylation in response to a variety of HORMONES and INTERCELLULAR SIGNALING PEPTIDES AND PROTEINS. Phosphorylation of RIBOSOMAL PROTEIN S6 by enzymes in this class results in increased expression of 5' top MRNAs. Although specific for RIBOSOMAL PROTEIN S6 members of this class of kinases can act on a number of substrates within the cell. The immunosuppressant SIROLIMUS inhibits the activation of ribosomal protein S6 kinases.
A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.
A non-essential amino acid occurring in natural form as the L-isomer. It is synthesized from GLYCINE or THREONINE. It is involved in the biosynthesis of PURINES; PYRIMIDINES; and other amino acids.
A protein-serine-threonine kinase that is activated by PHOSPHORYLATION in response to GROWTH FACTORS or INSULIN. It plays a major role in cell metabolism, growth, and survival as a core component of SIGNAL TRANSDUCTION. Three isoforms have been described in mammalian cells.
A group of protein-serine-threonine kinases that was originally identified as being responsible for the PHOSPHORYLATION of CASEINS. They are ubiquitous enzymes that have a preference for acidic proteins. Casein kinases play a role in SIGNAL TRANSDUCTION by phosphorylating a variety of regulatory cytoplasmic and regulatory nuclear proteins.
The uptake of naked or purified DNA by CELLS, usually meaning the process as it occurs in eukaryotic cells. It is analogous to bacterial transformation (TRANSFORMATION, BACTERIAL) and both are routinely employed in GENE TRANSFER TECHNIQUES.
The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments.
Identification of proteins or peptides that have been electrophoretically separated by blot transferring from the electrophoresis gel to strips of nitrocellulose paper, followed by labeling with antibody probes.
A mitogen-activated protein kinase kinase with specificity for JNK MITOGEN-ACTIVATED PROTEIN KINASES; P38 MITOGEN-ACTIVATED PROTEIN KINASES and the RETINOID X RECEPTORS. It takes part in a SIGNAL TRANSDUCTION pathway that is activated in response to cellular stress.
Products of proto-oncogenes. Normally they do not have oncogenic or transforming properties, but are involved in the regulation or differentiation of cell growth. They often have protein kinase activity.
Protein kinases that control cell cycle progression in all eukaryotes and require physical association with CYCLINS to achieve full enzymatic activity. Cyclin-dependent kinases are regulated by phosphorylation and dephosphorylation events.
A phorbol ester found in CROTON OIL which, in addition to being a potent skin tumor promoter, is also an effective activator of calcium-activated, phospholipid-dependent protein kinase (protein kinase C). Due to its activation of this enzyme, phorbol 12,13-dibutyrate profoundly affects many different biological systems.
A characteristic feature of enzyme activity in relation to the kind of substrate on which the enzyme or catalytic molecule reacts.
Any detectable and heritable change in the genetic material that causes a change in the GENOTYPE and which is transmitted to daughter cells and to succeeding generations.
An indolocarbazole that is a potent PROTEIN KINASE C inhibitor which enhances cAMP-mediated responses in human neuroblastoma cells. (Biochem Biophys Res Commun 1995;214(3):1114-20)
A group of compounds with the heterocyclic ring structure of benzo(c)pyridine. The ring structure is characteristic of the group of opium alkaloids such as papaverine. (From Stedman, 25th ed)
Proteins and peptides that are involved in SIGNAL TRANSDUCTION within the cell. Included here are peptides and proteins that regulate the activity of TRANSCRIPTION FACTORS and cellular processes in response to signals from CELL SURFACE RECEPTORS. Intracellular signaling peptide and proteins may be part of an enzymatic signaling cascade or act through binding to and modifying the action of other signaling factors.
A specific protein kinase C inhibitor, which inhibits superoxide release from human neutrophils (PMN) stimulated with phorbol myristate acetate or synthetic diacylglycerol.
Tumor-promoting compounds obtained from CROTON OIL (Croton tiglium). Some of these are used in cell biological experiments as activators of protein kinase C.
The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.
A transferase that catalyzes formation of PHOSPHOCREATINE from ATP + CREATINE. The reaction stores ATP energy as phosphocreatine. Three cytoplasmic ISOENZYMES have been identified in human tissues: the MM type from SKELETAL MUSCLE, the MB type from myocardial tissue and the BB type from nervous tissue as well as a mitochondrial isoenzyme. Macro-creatine kinase refers to creatine kinase complexed with other serum proteins.
A serine-threonine protein kinase that, when activated by DNA, phosphorylates several DNA-binding protein substrates including the TUMOR SUPPRESSOR PROTEIN P53 and a variety of TRANSCRIPTION FACTORS.
Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
A glycogen synthase kinase that was originally described as a key enzyme involved in glycogen metabolism. It regulates a diverse array of functions such as CELL DIVISION, microtubule function and APOPTOSIS.
Proteins prepared by recombinant DNA technology.
RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.
A group of enzymes that transfers a phosphate group onto an alcohol group acceptor. EC 2.7.1.
A cyclic AMP-dependent protein kinase subtype primarily found in particulate subcellular fractions. They are tetrameric proteins that contain two catalytic subunits and two type II-specific regulatory subunits.
Highly conserved protein-serine threonine kinases that phosphorylate and activate a group of AGC protein kinases, especially in response to the production of the SECOND MESSENGERS, phosphatidylinositol 3,4,-biphosphate (PtdIns(3,4)P2) and phosphatidylinositol 3,4,5-triphosphate (PtdIns(3,4,5)P3).
ATP:pyruvate 2-O-phosphotransferase. A phosphotransferase that catalyzes reversibly the phosphorylation of pyruvate to phosphoenolpyruvate in the presence of ATP. It has four isozymes (L, R, M1, and M2). Deficiency of the enzyme results in hemolytic anemia. EC
One of the mechanisms by which CELL DEATH occurs (compare with NECROSIS and AUTOPHAGOCYTOSIS). Apoptosis is the mechanism responsible for the physiological deletion of cells and appears to be intrinsically programmed. It is characterized by distinctive morphologic changes in the nucleus and cytoplasm, chromatin cleavage at regularly spaced sites, and the endonucleolytic cleavage of genomic DNA; (DNA FRAGMENTATION); at internucleosomal sites. This mode of cell death serves as a balance to mitosis in regulating the size of animal tissues and in mediating pathologic processes associated with tumor growth.
A class of cellular receptors that have an intrinsic PROTEIN-TYROSINE KINASE activity.
A group of phenyl benzopyrans named for having structures like FLAVONES.
The parts of a macromolecule that directly participate in its specific combination with another molecule.
Cells grown in vitro from neoplastic tissue. If they can be established as a TUMOR CELL LINE, they can be propagated in cell culture indefinitely.
A non-essential amino acid. In animals it is synthesized from PHENYLALANINE. It is also the precursor of EPINEPHRINE; THYROID HORMONES; and melanin.
A group of intracellular-signaling serine threonine kinases that bind to RHO GTP-BINDING PROTEINS. They were originally found to mediate the effects of rhoA GTP-BINDING PROTEIN on the formation of STRESS FIBERS and FOCAL ADHESIONS. Rho-associated kinases have specificity for a variety of substrates including MYOSIN-LIGHT-CHAIN PHOSPHATASE and LIM KINASES.
An essential amino acid occurring naturally in the L-form, which is the active form. It is found in eggs, milk, gelatin, and other proteins.
Recombinant proteins produced by the GENETIC TRANSLATION of fused genes formed by the combination of NUCLEIC ACID REGULATORY SEQUENCES of one or more genes with the protein coding sequences of one or more genes.
A group of enzymes removing the SERINE- or THREONINE-bound phosphate groups from a wide range of phosphoproteins, including a number of enzymes which have been phosphorylated under the action of a kinase. (Enzyme Nomenclature, 1992)
Any of the processes by which nuclear, cytoplasmic, or intercellular factors influence the differential control of gene action in enzyme synthesis.
Derivatives of the steroid androstane having two double bonds at any site in any of the rings.
A c-jun amino-terminal kinase that is activated by environmental stress and pro-inflammatory cytokines. Several isoforms of the protein with molecular sizes of 43 and 48 KD exist due to multiple ALTERNATIVE SPLICING.
The level of protein structure in which combinations of secondary protein structures (alpha helices, beta sheets, loop regions, and motifs) pack together to form folded shapes called domains. Disulfide bridges between cysteines in two different parts of the polypeptide chain along with other interactions between the chains play a role in the formation and stabilization of tertiary structure. Small proteins usually consist of only one domain but larger proteins may contain a number of domains connected by segments of polypeptide chain which lack regular secondary structure.
The relationship between the dose of an administered drug and the response of the organism to the drug.
A cell line derived from cultured tumor cells.
A protein serine-threonine kinase that catalyzes the PHOSPHORYLATION of I KAPPA B PROTEINS. This enzyme also activates the transcription factor NF-KAPPA B and is composed of alpha and beta catalytic subunits, which are protein kinases and gamma, a regulatory subunit.
The degree of similarity between sequences of amino acids. This information is useful for the analyzing genetic relatedness of proteins and species.
An enzyme that catalyzes the conversion of ATP and thymidine to ADP and thymidine 5'-phosphate. Deoxyuridine can also act as an acceptor and dGTP as a donor. (From Enzyme Nomenclature, 1992) EC
Benzo-indoles similar to CARBOLINES which are pyrido-indoles. In plants, carbazoles are derived from indole and form some of the INDOLE ALKALOIDS.
A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.
The phosphoric acid ester of serine.
A family of ribosomal protein S6 kinases that are structurally distinguished from RIBOSOMAL PROTEIN S6 KINASES, 70-KDA by their apparent molecular size and the fact they contain two functional kinase domains. Although considered RIBOSOMAL PROTEIN S6 KINASES, members of this family are activated via the MAP KINASE SIGNALING SYSTEM and have been shown to act on a diverse array of substrates that are involved in cellular regulation such as RIBOSOMAL PROTEIN S6 and CAMP RESPONSE ELEMENT-BINDING PROTEIN.
Immunologic method used for detecting or quantifying immunoreactive substances. The substance is identified by first immobilizing it by blotting onto a membrane and then tagging it with labeled antibodies.
Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.
A 195-kDa MAP kinase kinase kinase with broad specificity for MAP KINASE KINASES. It is found localized in the CYTOSKELETON and can activate a variety of MAP kinase-dependent pathways.
An enzyme that catalyzes the conversion of phosphatidylinositol (PHOSPHATIDYLINOSITOLS) to phosphatidylinositol 4-phosphate, the first committed step in the biosynthesis of phosphatidylinositol 4,5-bisphosphate.
Organic nitrogenous bases. Many alkaloids of medical importance occur in the animal and vegetable kingdoms, and some have been synthesized. (Grant & Hackh's Chemical Dictionary, 5th ed)
Cell lines whose original growing procedure consisted being transferred (T) every 3 days and plated at 300,000 cells per plate (J Cell Biol 17:299-313, 1963). Lines have been developed using several different strains of mice. Tissues are usually fibroblasts derived from mouse embryos but other types and sources have been developed as well. The 3T3 lines are valuable in vitro host systems for oncogenic virus transformation studies, since 3T3 cells possess a high sensitivity to CONTACT INHIBITION.
A family of cell cycle-dependent kinases that are related in structure to CDC28 PROTEIN KINASE; S CEREVISIAE; and the CDC2 PROTEIN KINASE found in mammalian species.
Any of the processes by which nuclear, cytoplasmic, or intercellular factors influence the differential control (induction or repression) of gene action at the level of transcription or translation.
The fission of a CELL. It includes CYTOKINESIS, when the CYTOPLASM of a cell is divided, and CELL NUCLEUS DIVISION.
An enzyme of the transferase class that uses ATP to catalyze the phosphorylation of diacylglycerol to a phosphatidate. EC
A family of highly conserved serine-threonine kinases that are involved in the regulation of MITOSIS. They are involved in many aspects of cell division, including centrosome duplication, SPINDLE APPARATUS formation, chromosome alignment, attachment to the spindle, checkpoint activation, and CYTOKINESIS.
Elements of limited time intervals, contributing to particular results or situations.
A 44 kDa mitogen-activated protein kinase kinase with specificity for MITOGEN-ACTIVATED PROTEIN KINASE 1 and MITOGEN-ACTIVATED PROTEIN KINASE 3.
An adenine nucleotide containing three phosphate groups esterified to the sugar moiety. In addition to its crucial roles in metabolism adenosine triphosphate is a neurotransmitter.
Serologic tests in which a positive reaction manifested by visible CHEMICAL PRECIPITATION occurs when a soluble ANTIGEN reacts with its precipitins, i.e., ANTIBODIES that can form a precipitate.
Transport proteins that carry specific substances in the blood or across cell membranes.
Proteins which bind to DNA. The family includes proteins which bind to both double- and single-stranded DNA and also includes specific DNA binding proteins in serum which can be used as markers for malignant diseases.
Proteins that control the CELL DIVISION CYCLE. This family of proteins includes a wide variety of classes, including CYCLIN-DEPENDENT KINASES, mitogen-activated kinases, CYCLINS, and PHOSPHOPROTEIN PHOSPHATASES as well as their putative substrates such as chromatin-associated proteins, CYTOSKELETAL PROTEINS, and TRANSCRIPTION FACTORS.
Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).
Theoretical representations that simulate the behavior or activity of biological processes or diseases. For disease models in living animals, DISEASE MODELS, ANIMAL is available. Biological models include the use of mathematical equations, computers, and other electronic equipment.
Intracellular fluid from the cytoplasm after removal of ORGANELLES and other insoluble cytoplasmic components.
An enzyme that phosphorylates myosin light chains in the presence of ATP to yield myosin-light chain phosphate and ADP, and requires calcium and CALMODULIN. The 20-kDa light chain is phosphorylated more rapidly than any other acceptor, but light chains from other myosins and myosin itself can act as acceptors. The enzyme plays a central role in the regulation of smooth muscle contraction.
The insertion of recombinant DNA molecules from prokaryotic and/or eukaryotic sources into a replicating vehicle, such as a plasmid or virus vector, and the introduction of the resultant hybrid molecules into recipient cells without altering the viability of those cells.
The biosynthesis of RNA carried out on a template of DNA. The biosynthesis of DNA from an RNA template is called REVERSE TRANSCRIPTION.
The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.
A family of calcium/calmodulin-dependent PROETIN-SERINE-THREONINE KINASES. They are ubiquitously expressed in adult and embryonic mammalian tissues, and their functions are tightly related to the early stages of eukaryotic programmed cell death.
The first continuously cultured human malignant CELL LINE, derived from the cervical carcinoma of Henrietta Lacks. These cells are used for VIRUS CULTIVATION and antitumor drug screening assays.
A negative regulatory effect on physiological processes at the molecular, cellular, or systemic level. At the molecular level, the major regulatory sites include membrane receptors, genes (GENE EXPRESSION REGULATION), mRNAs (RNA, MESSENGER), and proteins.
A cyclic GMP-dependent protein kinase subtype that is expressed in SMOOTH MUSCLE tissues and plays a role in regulation of smooth muscle contraction. Two isoforms, PKGIalpha and PKGIbeta, of the type I protein kinase exist due to alternative splicing of its mRNA.
Compounds of four rings containing a nitrogen. They are biosynthesized from reticuline via rearrangement of scoulerine. They are similar to BENZYLISOQUINOLINES. Members include chelerythrine and sanguinarine.
Domesticated bovine animals of the genus Bos, usually kept on a farm or ranch and used for the production of meat or dairy products or for heavy labor.
A regulatory calcium-calmodulin-dependent protein kinase that specifically phosphorylates CALCIUM-CALMODULIN-DEPENDENT PROTEIN KINASE TYPE 1; CALCIUM-CALMODULIN-DEPENDENT PROTEIN KINASE TYPE 2; CALCIUM-CALMODULIN-DEPENDENT PROTEIN KINASE TYPE 4; and PROTEIN KINASE B. It is a monomeric enzyme that is encoded by at least two different genes.
A mitogen-activated protein kinase kinase with specificity for P38 MITOGEN-ACTIVATED PROTEIN KINASES.
A structurally-diverse family of intracellular-signaling adaptor proteins that selectively tether specific protein kinase A subtypes to distinct subcellular sites. They play a role in focusing the PROTEIN KINASE A activity toward relevant substrates. Over fifty members of this family exist, most of which bind specifically to regulatory subunits of CYCLIC AMP-DEPENDENT PROTEIN KINASE TYPE II such as CAMP PROTEIN KINASE RIIALPHA or CAMP PROTEIN KINASE RIIBETA.
A non-receptor protein tyrosine kinase that is localized to FOCAL ADHESIONS and is a central component of integrin-mediated SIGNAL TRANSDUCTION PATHWAYS. Focal adhesion kinase 1 interacts with PAXILLIN and undergoes PHOSPHORYLATION in response to adhesion of cell surface integrins to the EXTRACELLULAR MATRIX. Phosphorylated p125FAK protein binds to a variety of SH2 DOMAIN and SH3 DOMAIN containing proteins and helps regulate CELL ADHESION and CELL MIGRATION.
Within a eukaryotic cell, a membrane-limited body which contains chromosomes and one or more nucleoli (CELL NUCLEOLUS). The nuclear membrane consists of a double unit-type membrane which is perforated by a number of pores; the outermost membrane is continuous with the ENDOPLASMIC RETICULUM. A cell may contain more than one nucleus. (From Singleton & Sainsbury, Dictionary of Microbiology and Molecular Biology, 2d ed)
A mitogen-activated protein kinase kinase with specificity for a subset of P38 MITOGEN-ACTIVATED PROTEIN KINASES that includes MITOGEN-ACTIVATED PROTEIN KINASE 12; MITOGEN-ACTIVATED PROTEIN KINASE 13; and MITOGEN-ACTIVATED PROTEIN KINASE 14.
Four carbon unsaturated hydrocarbons containing two double bonds.
Analysis of PEPTIDES that are generated from the digestion or fragmentation of a protein or mixture of PROTEINS, by ELECTROPHORESIS; CHROMATOGRAPHY; or MASS SPECTROMETRY. The resulting peptide fingerprints are analyzed for a variety of purposes including the identification of the proteins in a sample, GENETIC POLYMORPHISMS, patterns of gene expression, and patterns diagnostic for diseases.
Endogenous substances, usually proteins, which are effective in the initiation, stimulation, or termination of the genetic transcription process.
A serine threonine kinase that controls a wide range of growth-related cellular processes. The protein is referred to as the target of RAPAMYCIN due to the discovery that SIROLIMUS (commonly known as rapamycin) forms an inhibitory complex with TACROLIMUS BINDING PROTEIN 1A that blocks the action of its enzymatic activity.
A 38-kDa mitogen-activated protein kinase that is abundantly expressed in a broad variety of cell types. It is involved in the regulation of cellular stress responses as well as the control of proliferation and survival of many cell types. The kinase activity of the enzyme is inhibited by the pyridinyl-imidazole compound SB 203580.
Proteins which are found in membranes including cellular and intracellular membranes. They consist of two types, peripheral and integral proteins. They include most membrane-associated enzymes, antigenic proteins, transport proteins, and drug, hormone, and lectin receptors.
A family of non-receptor, PROLINE-rich protein-tyrosine kinases.
A c-jun amino-terminal kinase that is activated by environmental stress and pro-inflammatory cytokines. Several isoforms of the protein with molecular sizes of 48 and 54 KD exist due to multiple ALTERNATIVE SPLICING.
A heat-stable, low-molecular-weight activator protein found mainly in the brain and heart. The binding of calcium ions to this protein allows this protein to bind to cyclic nucleotide phosphodiesterases and to adenyl cyclase with subsequent activation. Thereby this protein modulates cyclic AMP and cyclic GMP levels.
The complex series of phenomena, occurring between the end of one CELL DIVISION and the end of the next, by which cellular material is duplicated and then divided between two daughter cells. The cell cycle includes INTERPHASE, which includes G0 PHASE; G1 PHASE; S PHASE; and G2 PHASE, and CELL DIVISION PHASE.
Linear POLYPEPTIDES that are synthesized on RIBOSOMES and may be further modified, crosslinked, cleaved, or assembled into complex proteins with several subunits. The specific sequence of AMINO ACIDS determines the shape the polypeptide will take, during PROTEIN FOLDING, and the function of the protein.
The process of moving proteins from one cellular compartment (including extracellular) to another by various sorting and transport mechanisms such as gated transport, protein translocation, and vesicular transport.
A broad category of carrier proteins that play a role in SIGNAL TRANSDUCTION. They generally contain several modular domains, each of which having its own binding activity, and act by forming complexes with other intracellular-signaling molecules. Signal-transducing adaptor proteins lack enzyme activity, however their activity can be modulated by other signal-transducing enzymes
A monomeric calcium-calmodulin-dependent protein kinase subtype that is expressed in a broad variety of mammalian cell types. Its expression is regulated by the action of CALCIUM-CALMODULIN-DEPENDENT PROTEIN KINASE KINASE. Several isoforms of this enzyme subtype are encoded by distinct genes.
Systems of enzymes which function sequentially by catalyzing consecutive reactions linked by common metabolic intermediates. They may involve simply a transfer of water molecules or hydrogen atoms and may be associated with large supramolecular structures such as MITOCHONDRIA or RIBOSOMES.
Genetically engineered MUTAGENESIS at a specific site in the DNA molecule that introduces a base substitution, or an insertion or deletion.
Electrophoresis in which a polyacrylamide gel is used as the diffusion medium.
Compounds or factors that act on a specific enzyme to increase its activity.
A monomeric calcium-calmodulin-dependent protein kinase subtype that is primarily expressed in neuronal tissues; T-LYMPHOCYTES and TESTIS. The activity of this enzyme is regulated by its phosphorylation by CALCIUM-CALMODULIN-DEPENDENT PROTEIN KINASE KINASE.
The sum of the weight of all the atoms in a molecule.
Ubiquitous, inducible, nuclear transcriptional activator that binds to enhancer elements in many different cell types and is activated by pathogenic stimuli. The NF-kappa B complex is a heterodimer composed of two DNA-binding subunits: NF-kappa B1 and relA.
Connective tissue cells which secrete an extracellular matrix rich in collagen and other macromolecules.
A type I cAMP-dependent protein kinase regulatory subunit that plays a role in confering CYCLIC AMP activation of protein kinase activity. It has a lower affinity for cAMP than the CYCLIC-AMP-DEPENDENT PROTEIN KINASE RIBETA SUBUNIT.
A subclass of phospholipases that hydrolyze the phosphoester bond found in the third position of GLYCEROPHOSPHOLIPIDS. Although the singular term phospholipase C specifically refers to an enzyme that catalyzes the hydrolysis of PHOSPHATIDYLCHOLINE (EC, it is commonly used in the literature to refer to broad variety of enzymes that specifically catalyze the hydrolysis of PHOSPHATIDYLINOSITOLS.
Small double-stranded, non-protein coding RNAs (21-31 nucleotides) involved in GENE SILENCING functions, especially RNA INTERFERENCE (RNAi). Endogenously, siRNAs are generated from dsRNAs (RNA, DOUBLE-STRANDED) by the same ribonuclease, Dicer, that generates miRNAs (MICRORNAS). The perfect match of the siRNAs' antisense strand to their target RNAs mediates RNAi by siRNA-guided RNA cleavage. siRNAs fall into different classes including trans-acting siRNA (tasiRNA), repeat-associated RNA (rasiRNA), small-scan RNA (scnRNA), and Piwi protein-interacting RNA (piRNA) and have different specific gene silencing functions.
A Janus kinase subtype that is involved in signaling from GROWTH HORMONE RECEPTORS; PROLACTIN RECEPTORS; and a variety of CYTOKINE RECEPTORS such as ERYTHROPOIETIN RECEPTORS and INTERLEUKIN RECEPTORS. Dysregulation of Janus kinase 2 due to GENETIC TRANSLOCATIONS have been associated with a variety of MYELOPROLIFERATIVE DISORDERS.
The span of viability of a cell characterized by the capacity to perform certain functions such as metabolism, growth, reproduction, some form of responsiveness, and adaptability.
The species Oryctolagus cuniculus, in the family Leporidae, order LAGOMORPHA. Rabbits are born in burrows, furless, and with eyes and ears closed. In contrast with HARES, rabbits have 22 chromosome pairs.
A 110-kDa extracellular signal-regulated MAP kinase that is activated in response to cellular stress and by GROWTH FACTOR RECEPTORS-mediated pathways.
The phosphoric acid ester of threonine. Used as an identifier in the analysis of peptides, proteins, and enzymes.
Guanosine cyclic 3',5'-(hydrogen phosphate). A guanine nucleotide containing one phosphate group which is esterified to the sugar moiety in both the 3'- and 5'-positions. It is a cellular regulatory agent and has been described as a second messenger. Its levels increase in response to a variety of hormones, including acetylcholine, insulin, and oxytocin and it has been found to activate specific protein kinases. (From Merck Index, 11th ed)
A eukayrotic protein serine-threonine phosphatase subtype that dephosphorylates a wide variety of cellular proteins. The enzyme is comprised of a catalytic subunit and regulatory subunit. Several isoforms of the protein phosphatase catalytic subunit exist due to the presence of multiple genes and the alternative splicing of their mRNAs. A large number of proteins have been shown to act as regulatory subunits for this enzyme. Many of the regulatory subunits have additional cellular functions.
A 6-kDa polypeptide growth factor initially discovered in mouse submaxillary glands. Human epidermal growth factor was originally isolated from urine based on its ability to inhibit gastric secretion and called urogastrone. Epidermal growth factor exerts a wide variety of biological effects including the promotion of proliferation and differentiation of mesenchymal and EPITHELIAL CELLS. It is synthesized as a transmembrane protein which can be cleaved to release a soluble active form.
An imidazole derivative which is a metabolite of the antineoplastic agents BIC and DIC. By itself, or as the ribonucleotide, it is used as a condensation agent in the preparation of nucleosides and nucleotides. Compounded with orotic acid, it is used to treat liver diseases.
Short sequences (generally about 10 base pairs) of DNA that are complementary to sequences of messenger RNA and allow reverse transcriptases to start copying the adjacent sequences of mRNA. Primers are used extensively in genetic and molecular biology techniques.
Proteins found in the nucleus of a cell. Do not confuse with NUCLEOPROTEINS which are proteins conjugated with nucleic acids, that are not necessarily present in the nucleus.
A long-acting derivative of cyclic AMP. It is an activator of cyclic AMP-dependent protein kinase, but resistant to degradation by cyclic AMP phosphodiesterase.
An enzyme that catalyzes the conversion of ATP and PHOSPHORYLASE B to ADP and PHOSPHORYLASE A.
A casein kinase that was originally described as a monomeric enzyme with a molecular weight of 30-40 kDa. Several ISOENZYMES of casein kinase I have been found which are encoded by separate genes. Many of the casein kinase I isoenzymes have been shown to play distinctive roles in intracellular SIGNAL TRANSDUCTION.
All of the processes involved in increasing CELL NUMBER including CELL DIVISION.
Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.
An amino acid that occurs in endogenous proteins. Tyrosine phosphorylation and dephosphorylation plays a role in cellular signal transduction and possibly in cell growth control and carcinogenesis.
The phenotypic manifestation of a gene or genes by the processes of GENETIC TRANSCRIPTION and GENETIC TRANSLATION.
The region of an enzyme that interacts with its substrate to cause the enzymatic reaction.
A specific inhibitor of phosphoserine/threonine protein phosphatase 1 and 2a. It is also a potent tumor promoter. (Thromb Res 1992;67(4):345-54 & Cancer Res 1993;53(2):239-41)
Organic compounds containing the -CN radical. The concept is distinguished from CYANIDES, which denotes inorganic salts of HYDROGEN CYANIDE.
The muscle tissue of the HEART. It is composed of striated, involuntary muscle cells (MYOCYTES, CARDIAC) connected to form the contractile pump to generate blood flow.
A 51-amino acid pancreatic hormone that plays a major role in the regulation of glucose metabolism, directly by suppressing endogenous glucose production (GLYCOGENOLYSIS; GLUCONEOGENESIS) and indirectly by suppressing GLUCAGON secretion and LIPOLYSIS. Native insulin is a globular protein comprised of a zinc-coordinated hexamer. Each insulin monomer containing two chains, A (21 residues) and B (30 residues), linked by two disulfide bonds. Insulin is used as a drug to control insulin-dependent diabetes mellitus (DIABETES MELLITUS, TYPE 1).
A serine-threonine kinase that plays important roles in CELL DIFFERENTIATION; CELL MIGRATION; and CELL DEATH of NERVE CELLS. It is closely related to other CYCLIN-DEPENDENT KINASES but does not seem to participate in CELL CYCLE regulation.
A positive regulatory effect on physiological processes at the molecular, cellular, or systemic level. At the molecular level, the major regulatory sites include membrane receptors, genes (GENE EXPRESSION REGULATION), mRNAs (RNA, MESSENGER), and proteins.
A key regulator of CELL CYCLE progression. It partners with CYCLIN E to regulate entry into S PHASE and also interacts with CYCLIN A to phosphorylate RETINOBLASTOMA PROTEIN. Its activity is inhibited by CYCLIN-DEPENDENT KINASE INHIBITOR P27 and CYCLIN-DEPENDENT KINASE INHIBITOR P21.
A mitogen-activated protein kinase kinase with specificity for JNK MITOGEN-ACTIVATED PROTEIN KINASES. It takes part in a SIGNAL TRANSDUCTION pathway that is activated in response to CYTOKINES.
Members of the class of compounds composed of AMINO ACIDS joined together by peptide bonds between adjacent amino acids into linear, branched or cyclical structures. OLIGOPEPTIDES are composed of approximately 2-12 amino acids. Polypeptides are composed of approximately 13 or more amino acids. PROTEINS are linear polypeptides that are normally synthesized on RIBOSOMES.
A species of the genus SACCHAROMYCES, family Saccharomycetaceae, order Saccharomycetales, known as "baker's" or "brewer's" yeast. The dried form is used as a dietary supplement.
Specific enzyme subunits that form the active sites of the type I and type II cyclic-AMP protein kinases. Each molecule of enzyme contains two catalytic subunits.
Two-ring crystalline hydrocarbons isolated from coal tar. They are used as intermediates in chemical synthesis, as insect repellents, fungicides, lubricants, preservatives, and, formerly, as topical antiseptics.
A 97-kDa extracellular signal-regulated MAP kinase. Mitogen-activated protein kinase 6 levels increase during cellular differentiation, while in proliferating cells the enzyme is degraded rapidly via the PROTEASOME ENDOPEPTIDASE COMPLEX.
Any of various enzymatically catalyzed post-translational modifications of PEPTIDES or PROTEINS in the cell of origin. These modifications include carboxylation; HYDROXYLATION; ACETYLATION; PHOSPHORYLATION; METHYLATION; GLYCOSYLATION; ubiquitination; oxidation; proteolysis; and crosslinking and result in changes in molecular weight and electrophoretic motility.
A type II cAMP-dependent protein kinase regulatory subunit that plays a role in confering CYCLIC AMP activation of protein kinase activity. It has a lower affinity for cAMP than the CYCLIC-AMP-DEPENDENT PROTEIN KINASE RIIALPHA SUBUNIT. Binding of this subunit by A KINASE ANCHOR PROTEINS may play a role in the cellular localization of type II protein kinase A.
Single-stranded complementary DNA synthesized from an RNA template by the action of RNA-dependent DNA polymerase. cDNA (i.e., complementary DNA, not circular DNA, not C-DNA) is used in a variety of molecular cloning experiments as well as serving as a specific hybridization probe.
Progressive restriction of the developmental potential and increasing specialization of function that leads to the formation of specialized cells, tissues, and organs.
A non-receptor protein-tyrosine kinase that is expressed primarily in the BRAIN; OSTEOBLASTS; and LYMPHOID CELLS. In the CENTRAL NERVOUS SYSTEM focal adhesion kinase 2 modulates ION CHANNEL function and MITOGEN-ACTIVATED PROTEIN KINASES activity.

Inducible NO synthase: role in cellular signalling. (1/16369)

The discovery of endothelium-derived relaxing factor and its identification as nitric oxide (NO) was one of the most exciting discoveries of biomedical research in the 1980s. Besides its potent vasodilatory effects, NO was found under certain circumstances to be responsible for the killing of microorganisms and tumour cells by activated macrophages and to act as a novel, unconventional type of neurotransmitter. In 1992, Science picked NO as the 'Molecule of the Year', and over the past years NO has become established as a universal intercellular messenger that acutely affects important signalling pathways and, on a more long-term scale, modulates gene expression in target cells. These actions will form the focus of the present review.  (+info)

JNK2 is required for efficient T-cell activation and apoptosis but not for normal lymphocyte development. (2/16369)

BACKGROUND: The Jun N-terminal kinase (JNK) signaling pathway has been implicated in cell proliferation and apoptosis, but its function seems to depend on the cell type and inducing signal. In T cells, JNK has been implicated in both antigen-induced activation and apoptosis. RESULTS: We generated mice lacking the JNK2 isozymes. The mutant mice were healthy and fertile but defective in peripheral T-cell activation induced by antibody to the CD3 component of the T-cell receptor (TCR) complex - proliferation and production of interleukin-2 (IL-2), IL-4 and interferon-gamma (IFN-gamma) were reduced. The proliferation defect was restored by exogenous IL-2. B-cell activation was normal in the absence of JNK2. Activation-induced peripheral T-cell apoptosis was comparable between mutant and wild-type mice, but immature (CD4(+) CD8(+)) thymocytes lacking JNK2 were resistant to apoptosis induced by administration of anti-CD3 antibody in vivo. The lack of JNK2 also resulted in partial resistance of thymocytes to anti-CD3 antibody in vitro, but had little or no effect on apoptosis induced by anti-Fas antibody, dexamethasone or ultraviolet-C (UVC) radiation. CONCLUSIONS: JNK2 is essential for efficient activation of peripheral T cells but not B cells. Peripheral T-cell activation is probably required indirectly for induction of thymocyte apoptosis resulting from administration of anti-CD3 antibody in vivo. JNK2 functions in a cell-type-specific and stimulus-dependent manner, being required for apoptosis of immature thymocytes induced by anti-CD3 antibody but not for apoptosis induced by anti-Fas antibody, UVC or dexamethasone. JNK2 is not required for activation-induced cell death of mature T cells.  (+info)

The Jun kinase 2 isoform is preferentially required for epidermal growth factor-induced transformation of human A549 lung carcinoma cells. (3/16369)

We have previously found that epidermal growth factor (EGF) mediates growth through the Jun N-terminal kinase/stress-activated kinase (JNK/SAPK) pathway in A549 human lung carcinoma cells. As observed here, EGF treatment also greatly enhances the tumorigenicity of A549 cells, suggesting an important role for JNK in cancer cell growth (F. Bost, R. McKay, N. Dean, and D. Mercola, J. Biol. Chem. 272:33422-33429, 1997). Several isoforms families of JNK, JNK1, JNK2, and JNK3, have been isolated; they arise from alternative splicing of three different genes and have distinct substrate binding properties. Here we have used specific phosphorothioate oligonucleotides targeted against the two major isoforms, JNK1 and JNK2, to discriminate their roles in EGF-induced transformation. Multiple antisense sequences have been screened, and two high-affinity and specific candidates have been identified. Antisense JNK1 eliminated steady-state mRNA and JNK1 protein expression with a 50% effective concentration (EC50) of <0.1 microM but did not alter JNK2 mRNA or protein levels. Conversely, antisense JNK2 specifically eliminated JNK2 steady-state mRNA and protein expression with an EC50 of 0.1 microM. Antisense JNK1 and antisense JNK2 inhibited by 40 and 70%, respectively, EGF-induced total JNK activity, whereas sense and scrambled-sequence control oligonucleotides had no effect. The elimination of mRNA, protein, and JNK activities lasted 48 and 72 h following a single Lipofectin treatment with antisense JNK1 and JNK2, respectively, indicating sufficient duration for examining the impact of specific elimination on the phenotype. Direct proliferation assays demonstrated that antisense JNK2 inhibited EGF-induced doubling of growth as well as the combination of active antisense oligonucleotides did. EGF treatment also induced colony formation in soft agar. This effect was completely inhibited by antisense JNK2 and combined-antisense treatment but not altered by antisense JNK1 alone. These results show that EGF doubles the proliferation (growth in soft agar as well as tumorigenicity in athymic mice) of A549 lung carcinoma cells and that the JNK2 isoform but not JNK1 is utilized for mediating the effects of EGF. This study represents the first demonstration of a cellular phenotype regulated by a JNK isoform family, JNK2.  (+info)

A novel genetic screen for snRNP assembly factors in yeast identifies a conserved protein, Sad1p, also required for pre-mRNA splicing. (4/16369)

The assembly pathway of spliceosomal snRNPs in yeast is poorly understood. We devised a screen to identify mutations blocking the assembly of newly synthesized U4 snRNA into a functional snRNP. Fifteen mutant strains failing either to accumulate the newly synthesized U4 snRNA or to assemble a U4/U6 particle were identified and categorized into 13 complementation groups. Thirteen previously identified splicing-defective prp mutants were also assayed for U4 snRNP assembly defects. Mutations in the U4/U6 snRNP components Prp3p, Prp4p, and Prp24p led to disassembly of the U4/U6 snRNP particle and degradation of the U6 snRNA, while prp17-1 and prp19-1 strains accumulated free U4 and U6 snRNA. A detailed analysis of a newly identified mutant, the sad1-1 mutant, is presented. In addition to having the snRNP assembly defect, the sad1-1 mutant is severely impaired in splicing at the restrictive temperature: the RP29 pre-mRNA strongly accumulates and splicing-dependent production of beta-galactosidase from reporter constructs is abolished, while extracts prepared from sad1-1 strains fail to splice pre-mRNA substrates in vitro. The sad1-1 mutant is the only splicing-defective mutant analyzed whose mutation preferentially affects assembly of newly synthesized U4 snRNA into the U4/U6 particle. SAD1 encodes a novel protein of 52 kDa which is essential for cell viability. Sad1p localizes to the nucleus and is not stably associated with any of the U snRNAs. Sad1p contains a putative zinc finger and is phylogenetically highly conserved, with homologues identified in human, Caenorhabditis elegans, Arabidospis, and Drosophila.  (+info)

Jun kinase phosphorylates and regulates the DNA binding activity of an octamer binding protein, T-cell factor beta1. (5/16369)

POU domain proteins have been implicated as key regulators during development and lymphocyte activation. The POU domain protein T-cell factor beta1 (TCFbeta1), which binds octamer and octamer-related sequences, is a potent transactivator. In this study, we showed that TCFbeta1 is phosphorylated following activation via the T-cell receptor or by stress-induced signals. Phosphorylation of TCFbeta1 occurred predominantly at serine and threonine residues. Signals which upregulate Jun kinase (JNK)/stress-activated protein kinase activity also lead to association of JNK with TCFbeta1. JNK associates with the activation domain of TCFbeta1 and phosphorylates its DNA binding domain. The phosphorylation of recombinant TCFbeta1 by recombinant JNK enhances the ability of TCFbeta1 to bind to a consensus octamer motif. Consistent with this conclusion, TCFbeta1 upregulates reporter gene transcription in an activation- and JNK-dependent manner. In addition, inhibition of JNK activity by catalytically inactive MEKK (in which methionine was substituted for the lysine at position 432) also inhibits the ability of TCFbeta1 to drive inducible transcription from the interleukin-2 promoter. These results suggest that stress-induced signals and T-cell activation induce JNK, which then acts on multiple cis sequences by modulating distinct transactivators like c-Jun and TCFbeta1. This demonstrates a coupling between the JNK activation pathway and POU domain proteins and implicates TCFbeta1 as a physiological target in the JNK signal transduction pathway leading to coordinated biological responses.  (+info)

Functions of cyclin A1 in the cell cycle and its interactions with transcription factor E2F-1 and the Rb family of proteins. (6/16369)

Human cyclin A1, a newly discovered cyclin, is expressed in testis and is thought to function in the meiotic cell cycle. Here, we show that the expression of human cyclin A1 and cyclin A1-associated kinase activities was regulated during the mitotic cell cycle. In the osteosarcoma cell line MG63, cyclin A1 mRNA and protein were present at very low levels in cells at the G0 phase. They increased during the progression of the cell cycle and reached the highest levels in the S and G2/M phases. Furthermore, the cyclin A1-associated histone H1 kinase activity peaked at the G2/M phase. We report that cyclin A1 could bind to important cell cycle regulators: the Rb family of proteins, the transcription factor E2F-1, and the p21 family of proteins. The in vitro interaction of cyclin A1 with E2F-1 was greatly enhanced when cyclin A1 was complexed with CDK2. Associations of cyclin A1 with Rb and E2F-1 were observed in vivo in several cell lines. When cyclin A1 was coexpressed with CDK2 in sf9 insect cells, the CDK2-cyclin A1 complex had kinase activities for histone H1, E2F-1, and the Rb family of proteins. Our results suggest that the Rb family of proteins and E2F-1 may be important targets for phosphorylation by the cyclin A1-associated kinase. Cyclin A1 may function in the mitotic cell cycle in certain cells.  (+info)

The bystander effect in the HSVtk/ganciclovir system and its relationship to gap junctional communication. (7/16369)

The bystander effect (BSE) is an interesting and important property of the herpes thymidine kinase/ganciclovir (hTK/GCV) system of gene therapy for cancer. With the BSE, not only are the hTK expressing cells killed upon ganciclovir (GCV) exposure but also neighboring wild-type tumor cells. On testing a large number of tumor cell lines in vitro, a wide range of sensitivity to bystander killing was found. Since transfer of toxic GCV metabolites from hTK-modified to wild-type tumor cells via gap junctions (GJ) seemed to be a likely mechanism of the BSE, we tested GJ function in these various tumors with a dye transfer technique and pharmacological agents known to affect GJ communication. We confirmed that mixtures of tumor cell resistant to the BSE did not show dye transfer from cell to cell while bystander-sensitive tumor cells did. Dieldrin, a drug known to decrease GJ communication, diminished dye transfer and also inhibited the BSE. Forskolin, an upregulator of cAMP did increase GJ, but directly inhibited hTK and therefore its effect on BSE could not be determined. We conclude that these observations further support port the concept that functional GJ play an important role in the BSE and further suggest that pharmacological manipulation of GJ may influence the outcome of cancer therapy with hTK/GCV.  (+info)

Herpes virus induced proteasome-dependent degradation of the nuclear bodies-associated PML and Sp100 proteins. (8/16369)

The PML protein is associated to nuclear bodies (NBs) whose functions are as yet unknown. PML and two other NBs-associated proteins, Sp100 And ISG20 are directly induced by interferons (IFN). PML and Sp100 proteins are covalently linked to SUMO-1, and ubiquitin-like peptide. PML NBs are disorganized in acute promyelocytic leukemia and during several DNA virus infections. In particular, the HSV-1 ICP0 protein is known to delocalize PML from NBs. Thus, NBs could play an important role in oncogenesis, IFN response and viral infections. Here, we show that HSV-1 induced PML protein degradation without altering its mRNA level. This degradation was time- and multiplicity of infection-dependent. Sp100 protein was also degraded, while another SUMO-1 conjugated protein, RanGAP1 and the IFN-induced protein kinase PKR were not. The proteasome inhibitor MG132 abrogated the HSV-1-induced PML and Sp100 degradation and partially restored their NB-localization. HSV-1 induced PML and Sp100 degradation constitutes a new example of viral inactivation of IFN target gene products.  (+info)

Niles, R M. and Logue, M P., Retinoid acid increases cyclic amp-dependent protein kinase activity in b16-f1 mouse melanoma cells. Abstr. (1979). Subject Strain Bibliography 1979. 1639 ...
Phytopathology 92:75-80...Phytopathology 92:75-80...A Point Mutation in the Two-Component Histidine Kinase BcOS-1 Gene Confers Dicarboximide Resistance in Field Isolates of Botrytis cinerea...Michiyo Oshima , Makoto Fujimura , Shinpei Banno , Chigusa Hashimoto , Takayuki Motoyama , Akihiko Ichiishi , and Isamu Yamaguchi...
Protein Kinase C (PKC) is a family of nucleotide-independent, Ca2+-dependent serine kinases. ,ref name=na,Takai, Y., Kishimoto, A., Inoue, M., & Nishizuka, Y. (1977). Studies on a cyclic nucleotide-independent protein kinase and its proenzyme in mammalian tissues. I. Purification and characterization of an active enzyme from bovine cerebellum. J. Biol. Chem., 252(21), 7603-7609. [] ,/ref,. At least 11 isozymes have been identified, ,ref name=peter,Acs, P., Wang, Q., Bogi, K., Marquez, A., Lorenzo, P., Biro, T., Szallai, Z., Mushinski, F., & Blue, P. (1997). Both the Catalytic and Regulatory Domains of Protein Kinase C Chimeras Modulate the Proliferative Properties of NIH 3T3 Cells. J Biol Chem., 272(45), 28793-28799. Retrieved May 15, 2009, from [ Pubmed],/ref, most PKC isozymes are ubiquitous and multiple members of the ...
Protein Kinase C (PKC) is a family of nucleotide-independent, Ca2+-dependent serine kinases. ,ref name=na,Takai, Y., Kishimoto, A., Inoue, M., & Nishizuka, Y. (1977). Studies on a cyclic nucleotide-independent protein kinase and its proenzyme in mammalian tissues. I. Purification and characterization of an active enzyme from bovine cerebellum. J. Biol. Chem., 252(21), 7603-7609. [] ,/ref,. At least 11 isozymes have been identified, ,ref name=peter,Acs, P., Wang, Q., Bogi, K., Marquez, A., Lorenzo, P., Biro, T., Szallai, Z., Mushinski, F., & Blue, P. (1997). Both the Catalytic and Regulatory Domains of Protein Kinase C Chimeras Modulate the Proliferative Properties of NIH 3T3 Cells. J Biol Chem., 272(45), 28793-28799. Retrieved May 15, 2009, from [ Pubmed],/ref, most PKC isozymes are ubiquitous and multiple members of the ...
The subcellular distribution of protein kinase activity in isolated islets of Langerhans was determined. The majority (70%) of cyclic AMP-dependent protein kinase activity was located in the S-100 (soluble) fraction, while the majority (42%) of cyclic AMP-independent activity was located in the solublised P-100 (containing mitochondria, secretory granules and microsomes) fraction. Partial characterisation of the islet cyclic AMP-dependent protein kinase activity revealed the presence of two isozymes designated Type I and Type II. Type II kinase was the predominant isozyme of the S-100 fraction and Type I was the predominant isozyme found in the solublised P-100 fraction. Nonidet-P40 (a non-ionic detergent) was found to activate the S-100 cyclic AMP-dependent protein kinase activity, although no significant increase in protein kinase activity was observed when the P-0.6 (containing nuclei and cellular debris) fraction and P-100 fraction were solublised with Nonidet-P40. This activation was ...
TY - JOUR. T1 - Phosphorylation of cardiac troponin by guanosine 3. T2 - 5-monophosphate-dependent protein kinase. AU - Blumenthal, D. K.. AU - Stull, J. T.. AU - Gill, G. N.. PY - 1978. Y1 - 1978. N2 - Homogeneous cGMP-dependent protein kinase catalyzes the rapid incorporation of phosphate, specifically into the inhibitory subunit of purified cardiac troponin with a maximal incorporation of 1 mol of phosphate/mol of troponin. When troponin was incubated in the presence of both cGMP- and cAMP-dependent protein kinases, a maximal incorporation of 1 mol of phosphate/mol of troponin was observed which suggested phosphorylation of the same site by the two kinases. Both cyclic nucleotide-dependent kinases had similar K(m) values for troponin, but the V(max) value for the phosphorylation reaction catalyzed by cAMP-dependent protein kinase was 12-fold greater than the value obtained for cGMP-dependent protein kinase.. AB - Homogeneous cGMP-dependent protein kinase catalyzes the rapid incorporation of ...
Shop Leucine-rich repeat receptor protein kinase ELISA Kit, Recombinant Protein and Leucine-rich repeat receptor protein kinase Antibody at MyBioSource. Custom ELISA Kit, Recombinant Protein and Antibody are available.
Nov 02, 2019 (Eon Market Research via COMTEX) -- The market report, titled Global Serine/Threonine Protein Kinase Chk1 Market Research Report 2019 - By Manufacturers, Product Type, Applications, Region and Forecast to 2026′, recently added to the market research repository of, details in-depth past and present analytical and statistical data about the global Serine/Threonine Protein Kinase Chk1 market. The report describes the Serine/Threonine Protein Kinase Chk1 market in detail in terms of the economic and regulatory factors that are currently shaping the markets growth trajectory, the regional segmentation of the global Serine/Threonine Protein Kinase Chk1 market , and an analysis of the markets downstream and upstream value and supply chains. Competitive Research of Global Serine/Threonine Protein Kinase Chk1 Market 2019 Based on Key Players: CanBas Co Ltd Cascadian Therapeutics Inc Eli Lilly and Company Genentech Inc ProNAi Therapeutics Inc Sareum Holdings Plc ...
Antimicrobial resistance is a major societal problem as there are resistant bacteria to any antibiotic available, and they spread across countries and continents. For this a novel antibacterial medicine with a low potential of resistance development is urgently needed. Researchers from Spain, The Netherlands, and United Kingdom have joined efforts to identify bacterial histidine kinase inhibitors that can be further developed as novel antibacterial medicines.
An antiserum against the catalytic subunit C of cyclic AMP-dependent protein kinase, isolated from bovine heart type II protein kinase, was produced in rabbits. Reaction of the catalytic subunit with antiserum and separation of the immunoglobulin G fraction by Protein A-Sepharose quantitatively removed the enzyme from solutions. Comparative immunotitration of protein kinases showed that the amount of antiserum required to eliminate 50% of the enzymic activity was identical for pure catalytic subunit, and for holoenzymes type I and type II. The reactivity of the holoenzymes with the antiserum was identical in the absence or the presence of dissociating concentrations of cyclic AMP. Most of the holoenzyme (type II) remains intact when bound to the antibodies as shown by quantification of the regulatory subunit in the supernatant of the immunoprecipitate. Titration with the antibodies also revealed the presence of a cyclic AMP-independent histone kinase in bovine heart protein kinase I preparations ...
PubMed comprises more than 30 million citations for biomedical literature from MEDLINE, life science journals, and online books. Citations may include links to full-text content from PubMed Central and publisher web sites.
The occurrence of endogenous substrate proteins for Ca2+-dependent protein kinase, augmented by either phospholipid or calmodulin, and for cyclic AMP-dependent protein kinase was examined in homogenates and subcellular fractions of mouse pancreatic islets. Islet protein phosphorylation was enhanced by Ca2+-calmodulin; the major endogenous substrates in the homogenate were two proteins of Mr 53000 and 100000. The Mr-100000 phosphoprotein was localized to a 27000g-supernatant fraction, whereas the Mr-53000 phosphoprotein was present in a 27000g particulate fraction of mouse islets. In the presence of Ca2+, phosphatidylserine stimulated phosphorylation of 15 proteins, of Mr 17000-190000, in a 27000g-supernatant fraction. No effects of Ca2+ plus phosphatidylserine were observed in a 27000g particulate fraction of mouse islets. Examination of cyclic AMP-dependent protein phosphorylation revealed five substrate proteins, of Mr 23000-72000, present in the 27000g supernatant of mouse islets. No common ...
Marco Albanese recently presented a poster on using fragment-based approaches to discover compounds targeting the ATP-binding domain of bacterial histidine kinases at the 7th RSC-BMCS Fragment-based Drug Discovery meeting in Cambridge. Bacterial histidine kinases (HKs) are part of two-component systems (TCSs), the most widespread means by which bacteria sense and adapt to external and internal stimuli. […]. ...
Werner, C.G., Godrey, V., Arnold, R.R., Featherstone, G.L., Bender, D., Schlossmann, Jens, Schiemann, M., Hofmann, F. and Pryzwansky, K.B. (2005) Neutrophil dysfunction in guanosine 3,5-cyclic monophosphate-dependent protein kinase I-deficient mice. Journal of Immunology 175, pp. 1919-1929 ...
Lung cancer results when normal check and balance system of cell division is disrupted and ultimately the cells divide and proliferate in an uncontrollable manner forming a mass of cells in our body, known as tumor. Frequent mutations in Protein Kinase Domain alter the process of phosphorylation which results in abnormality in regulations of cell apoptosis and differentiation. Tyrosine Protein kinases and Serine/Threonine Protein Kinases are the two broad classes of protein kinases in accordance to their substrate specificity. The study of Tyrosine protein kinase and serine Kinase coding regions have the importance of sequence and structure determinants of cancer-causing mutations from mutation-dependent activation process. In the present study, we analyzed huge amounts of data extracted from various biological databases and NCBI. Out of the 534 proteins that may play a role in lung cancer, 71 proteins were selected that are likely to be actively involved in lung cancer. These proteins were evaluated by
We have expressed Arabidopsis homologs of MEK and MAPK in E. coli and purified them to apparent homogeneity using affinity chromatography. Consistent with their similarity to other protein kinases, both possess intrinsic protein kinase activity, as determined by in vitro phosphorylation assays. Purified, recombinant AtMEK1 was able to phosphorylate and activate ATMPK4 in vitro, which indicates that a plant MEK homolog is able to phosphorylate and activate a MAPK from plants.. Activation of animal MAPK is achieved by phosphorylation of both Tyr and Thr by the dual-specificity kinase MEK. Similarly, in order for ATMPK4 to be highly active requires phosphorylation of both Tyr and Thr residues, as demonstrated using phospho-Tyr-specific phosphatases and antibodies. This is consistent with the findings of Ádám et al. (1997), who utilized an animal Tyr phosphatase to demonstrate that Tyr phosphorylation is required for full activity of a myelin basic protein kinase from harpin-treated tobacco ...
Since the publication of Protein Kinases in 1994 many novel protein kinases have been discovered, but perhaps more importantly there have been dramatic advances in our understanding of the cellular functions of this remarkably diverse class of proteins. Protein Kinase Functions is not just an update of the previous edition but provides a new focus on the context and function of protein kinases, thus reflecting the recent advances in kinase biology.
TY - JOUR. T1 - Detection of protein kinase homologues and viral RNA-binding domains utilizing polyclonal antiserum prepared against a baculovirus-expressed ds RNA-activated 68,000-Da protein kinase. AU - Barber, Glen N.. AU - Tomita, Judy. AU - Garfinkel, Michele S.. AU - Meurs, Eliane. AU - Hovanessian, Ara. AU - Katze, Michael G.. PY - 1992/12. Y1 - 1992/12. N2 - The P68 protein kinase (referred to as P68 based on its Mr of 68,000 in human cells) is a serine/threonine kinase induced by interferon treatment and activated by dsRNAs. The kinase is under tight controls in virus-infected cells since once activated, it phosphorylates its natural substrate eukaryotic initiation factor 2 (elF-2), leading to potential limitations in functional elF-2 and decreases in protein synthesis initiation. To further delineate the molecular mechanisms underlying kinase regulation, we attempted to express the P68 protein kinase in insect cells using a baculovirus vector. Repeated efforts to isolate recombinant ...
Shop Probable receptor-like protein kinase ELISA Kit, Recombinant Protein and Probable receptor-like protein kinase Antibody at MyBioSource. Custom ELISA Kit, Recombinant Protein and Antibody are available.
Protein kinase function is evolutionarily conserved from Escherichia coli to human [(PUBMED:12471243)]. Protein kinases play a role in a multitude of cellular processes, including division, proliferation, apoptosis, and differentiation [(PUBMED:12368087)]. Phosphorylation usually results in a functional change of the target protein by changing enzyme activity, cellular location, or association with other proteins. The catalytic subunits of protein kinases are highly conserved, and several structures have been solved [(PUBMED:15078142)], leading to large screens to develop kinase-specific inhibitors for the treatments of a number of diseases [(PUBMED:15320712)].. Eukaryotic protein kinases [(PUBMED:12734000), (PUBMED:7768349), (PUBMED:1835513), (PUBMED:1956325), (PUBMED:3291115)] are enzymes that belong to a very extensive family of proteins which share a conserved catalytic core common with both serine/threonine and tyrosine protein kinases. There are a number of conserved regions in the ...
Protein kinase function is evolutionarily conserved from Escherichia coli to human [(PUBMED:12471243)]. Protein kinases play a role in a multitude of cellular processes, including division, proliferation, apoptosis, and differentiation [(PUBMED:12368087)]. Phosphorylation usually results in a functional change of the target protein by changing enzyme activity, cellular location, or association with other proteins. The catalytic subunits of protein kinases are highly conserved, and several structures have been solved [(PUBMED:15078142)], leading to large screens to develop kinase-specific inhibitors for the treatments of a number of diseases [(PUBMED:15320712)].. Eukaryotic protein kinases [(PUBMED:12734000), (PUBMED:7768349), (PUBMED:1835513), (PUBMED:1956325), (PUBMED:3291115)] are enzymes that belong to a very extensive family of proteins which share a conserved catalytic core common with both serine/threonine and tyrosine protein kinases. There are a number of conserved regions in the ...
The KinG database is a comprehensive collection of serine/threonine/tyrosine-specific kinases and their homologues identified in various completed genomes using sequence and profile search methods. The database hosted at http://hodgkin. provides the amino acid sequences, functional domain assignments and classification of gene products containing protein kinase domains. A search tool enabling the retrieval of protein kinases with specified subfamily and domain combinations is one of the key features of the resource. Identification of a kinase catalytic domain in the users query sequence is possible using another search tool. The occurrence and location of critical catalytic residues if the query has a catalytic kinase domain, recognition of non-kinase domains in the sequence and subfamily classification of the kinase in the query will help in deciphering the biological role of the kinase. This online compilation can also be used to compare the protein kinases of a given ...
Purpose : Protein kinases play an important role in several cell processes such as proliferation, transcription, and pathologic changes. Kinase inhibitors have thus been proposed for treatment against diseases including cancer. In ophthalmology, ROCK inhibitor has already been launched as an antiglaucoma drug in Japan. However, discovery of small molecule inhibitors for specific protein kinases is still challenging. This is because approximately 500 protein kinases exist and more than 2,000 other purine-binding proteins share similar ATP binding pockets of kinases. The purpose of this study was to develop an in silico method for identifying potential kinase inhibitors, and the anticancer drug axitinib was used as a representative kinase inhibitor. Methods : Sequences for 9 typical kinases were compared to VEGFR tyrosine kinase, the three amino acid sequences on the hinge region of each kinase were identified, and the surfaces of the ATP binding cavities in the kinases were analyzed in silico ...
TY - JOUR. T1 - Partial fractionation and characterization of nuclear protein kinases in HeLa S3 cells. AU - Thomson, Judith A.. AU - Mon, Manuel J.. AU - Stein, Janet L.. AU - Duval, Kathryn A.. AU - Kleinsmith, Lewis J.. AU - Stein, Gary S.. PY - 1979/8. Y1 - 1979/8. N2 - Five fractions of phosphoprotein kinase activity were separated by phosphocellulose chromatography of nuclear non-histone phosphoproteins isolated from exponentially-growing HeLa S3 cells. Each fraction contained a heterogeneous group of proteins and possibly more than one protein kinase. These fractions were characterized with respect to specific activity and optimal concentrations of Mg2+ and Mn2+. The ability of each kinase fraction to catalyze the incorporation of 32P from [γ-32P]ATP into various molecular weight classes of heat-inactivated non-histone nuclear phosphoproteins (as substrate) was examined by electrophoretically resolving the proteins in SDS-polyacrylamide gels. Each kinase fraction induced a distinctive ...
The kinase complement of the human genome, the kinome, provided a start point for comprehensive investigation of protein phosphorylation. Manning et al. identified 518 protein kinase genes and 106 protein kinase pseudogenes in human (Manning et al., 2002 Science). Most protein kinases contain a conserved catalytic domain belonging to the eukaryotic protein kinase (ePK) superfamily (all other protein kinases are classified as atypical protein kinases, or aPKs). ePKs are classified into 7 major groups, including AGC, CAMK, CK1, CMGC, STE, TK, and TKL, and are subdivided into families, and sometimes subfamilies, based on the sequence of their ePK domains. All 518 human kinases are listed as following, users can clikc into the URL link to investigate the detail information about the kinase and their substrates. ...
In recent years, members of the protein kinase family have been discovered at an accelerated pace. Most were first described, not through the traditional biochemical approach of protein purification and enzyme assay, but as putative protein kinase amino acid sequences deduced from the nucleotide sequences of molecularly cloned genes or complementary DNAs. Phylogenetic mapping of the conserved protein kinase catalytic domains can serve as a useful first step in the functional characterization of these newly identified family members. ...
Antibodies raised against the protein encoded by a lacZ-CDC28 in-frame fusion were shown to immunoprecipitate the CDC28 product from yeast cell lysates. The polypeptide p36CDC28 is a phosphoprotein of apparent Mr 36,000. Immune complexes prepared from yeast cell lysates by using anti-CDC28 antibody were found to possess a protein kinase activity, as determined by the transfer of label from [gamma-32P]ATP to a coprecipitated Mr 40,000 protein of unknown identity or function (p40). This activity was absent or thermolabile when extracts were prepared from several different cdc28 temperature-sensitive strains. The protein kinase activity was dependent on Zn2+ and transferred phosphate specifically to serine and threonine residues.
Video articles in JoVE about radioactive waste include Metabolic Labeling of Leucine Rich Repeat Kinases 1 and 2 with Radioactive Phosphate, Quantification of Bacterial Histidine Kinase Autophosphorylation Using a Nitrocellulose Binding Assay, Radioactive in situ Hybridization for Detecting Diverse Gene Expression Patterns in Tissue, Methods for the Determination of Rates of Glucose and Fatty Acid Oxidation in the Isolated Working Rat Heart, Analysis of Protein Import into Chloroplasts Isolated from Stressed Plants, Specificity Analysis of Protein Lysine Methyltransferases Using SPOT Peptide Arrays, Studying Ribonucleotide Incorporation: Strand-specific Detection of Ribonucleotides in the Yeast Genome and Measuring Ribonucleotide-induced Mutagenesis, Murine Lymphocyte Labeling by 64Cu-Antibody Receptor Targeting for In Vivo Cell Trafficking by PET/CT, Oligopeptide Competition Assay for Phosphorylation Site Determination, Isolation and Chemical Characterization of Lipid A from Gram
TY - JOUR. T1 - ERK3 is a constitutively nuclear protein kinase. AU - Cheng, Mangeng. AU - Boulton, Teri G.. AU - Cobb, Melanie H.. PY - 1996/4/12. Y1 - 1996/4/12. N2 - The ERK3 cDNA predicts a protein of 62,000 in size with a C-terminal domain that extends 180 amino acids beyond the conserved core of ERK family protein kinases. Immunoblotting with antibodies raised to recombinant protein and to peptides from the catalytic core and three regions of the C-terminal tail revealed that ERK3 is the expected size and is ubiquitously expressed in a variety of cell lines and tissues. ERK3, unlike the MAP kinases ERK1 and ERK2, is localized in the nucleus in exponentially growing, quiescent, and growth factor-stimulated cells. If the 180 amino acids at its C terminus are deleted, the resulting ERK3 fragment of 45 kDa is still found primarily in the nucleus, indicating that the C terminus is not required for its localization. Recombinant ERK3 expressed in mammalian cells or in bacteria is a protein ...
Neurodegenerative disorders (Alzheimers, Parkinsons and Huntingtons disease) are characterised by the irreversible loss of nerve cell function. Protein kinases such as JNK and LRRK2 are major players in neurodegenerative disorders, however their mechanism of action is largely unknown. Even though our understanding of the physiological functions of these molecules is in its infancy. drug targeting strategies are already underway. Our lab uses a proteomics screen developed in the lab to identify protein kinase substrates. The identification of novel targets combined with biochemical, genetic and imaging approaches has revealed unexpected functions for kinases in neocortical development and provided mechanistic insight in neuronal disease ...
Identifying the substrates of protein kinases to understand their modes of action has been undertaken by various approaches and remains an ongoing challenge
contains similarity to Pfam domain PF00069 (Protein kinase domain)contains similarity to Interpro domains IPR002290 (Serine/threonine protein kinase), IPR008271 (Serine/threonine protein kinase, active site), IPR000719 (Protein kinase), IPR001245 (Tyrosine protein kinase ...
Recombinant c-AMP dependant Protein Kinase A regulatory subunit 2 alpha from Prospec cat# pka-204. ProteoGenix provides you the best Kinases proteins.Shop now from our 200 000 + products.
Protein phosphorylation is known to play an important role in various cellular processes such as cell division, metabolism, survival and apoptosis. It is driven by specific enzymes, tyrosine and serine-threonine protein kinases. Human protein kinases constitute a complicated system with intricate in …
Protein kinases in human leukemic cells.: Protein kinase activities and cyclic AMP binding capacity were investigated in human peripheral blood cells from leuke
Histidine protein kinases (HPKs) are a large family of signal-transduction enzymes that autophosphorylate on a conserved histidine residue. HPKs form two-component signaling systems together with their downstream target proteins, the response regulators, which have a conserved aspartate in a so-called receiver domain that is phosphorylated by the HPK. Two-component signal transduction is prevalent in bacteria and is also widely used by eukaryotes outside the animal kingdom. The typical HPK is a transmembrane receptor with an amino-terminal extracellular sensing domain and a carboxy-terminal cytosolic signaling domain; most, if not all, HPKs function as dimers. They show little similarity to protein kinases that phosphorylate serine, threonine or tyrosine residues, but may share a distant evolutionary relationship with these enzymes. In excess of a thousand known genes encode HPKs, which are important for multiple functions in bacteria, including chemotaxis and quorum sensing, and in eukaryotes,
In the yeast, Saccharomyces cerevesiae, phosphorelay signaling systems that involve a three-step His-Asp-His-Asp phosphotransfer are involved in transmitting signals in response to cellular stress. The animation shows one example of such a phosphorelay system involved in yeast responses to changes in osmolarity. Under conditions of low osmolarity, a histidine-aspartate phosphorelay pathway transmits information that deactivates one signaling pathway and activates gene expression through another pathway. In response to high osmolarity, the Sln1 kinase that initiates the phosphorelay is inhibited and the Hog1 mitogen-activated protein kinase cascade is active. ...
The broad goal of this proposal is to understand mechanisms for synaptic plasticity that may underlie aspects of learning and memory, especially for regulation...
Mitogen activated protein kinases (MAPKs) are serine-threonine protein kinases that play critical roles in regulating cellular homeostasis. MAPKs are members of...
contains similarity to Pfam domain PF00069 (Protein kinase domain)contains similarity to Interpro domains IPR002290 (Serine/threonine protein kinase), IPR008271 (Serine/threonine protein kinase, active site), IPR000719 (Protein kinase ...
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Cyclic AMP-dependent protein kinase has been well established to be composed of catalytic and regulatory subunits, and cyclic AMP acts to dissociate these subun
SWISS-MODEL Template Library (SMTL) entry for 5nk7.1. Crystal Structure of Ephrin A2 (EphA2) Receptor Protein Kinase with Compound 2a
Full-length recombinant human PRKX was expressed by baculovirus in Sf9 insect cells using an N-terminal GST tag. PRKX is a serine/threonine protein kinase that is closely related to the catalytic subunit of the cAMP-dependent protein kinase.
Full-length recombinant human PRKX was expressed by baculovirus in Sf9 insect cells using an N-terminal GST tag. PRKX is a serine/threonine protein kinase that is closely related to the catalytic subunit of the cAMP-dependent protein kinase.
Complement factor C3, recently found to contain covalently bound phosphate, was phosphorylated in vitro by cyclic AMP-dependent protein kinase (protein kinase A) and Ca2+-activated, phospholipid-dependent protein kinase (protein kinase C). Both protein kinases phosphorylated the same serine residue(s) located in the C3a portion of the alpha-chain. In addition, protein kinase C phosphorylated the beta-chain to a lesser extent. Protein kinase A gave a maximal incorporation of 1 mol of phosphate/mol of C3 while that value with protein kinase C was 1.5 mol of phosphate/mol of C3. The velocity in pmol of [32P]phosphate/(min x unit kinase) was 20 times higher for protein kinase C than for protein kinase A although a 10 times lower ratio of protein kinase to C3 was used in the former case. The apparent Kmfor C3 was 2.6 µM when protein kinase C was used. The phosphorylated C3 was found to be more resistant to partial degradation by trypsin than unphosphorylated C3. It was also found that ...
TY - JOUR. T1 - Phosphorylation of tyrosine hydroxylase by cyclic GMP - Dependent protein kinase. AU - Roskoski, R.. AU - Vulliet, Philip R. AU - Glass, D. B.. PY - 1987. Y1 - 1987. N2 - Tyrosine hydroxylase purified from rat pheochromycytoma was phosphorylated and activated by purified cyclic GMP-dependent protein kinase as well as by cyclic AMP-dependent protein kinase catalytic subunit. The extent of activation was correlated with the degree of phosphate incorporated into the enzyme. Comparable stoichiometric ratios (0.6 mol phosphate/mol tyrosine hydroxylase subunit) were obtained at maximal concentrations of either cyclic AMP-dependent or cyclic GMP-dependent protein kinases. The enzymes appeared to mediate the phosphorylation of the same residue based on the observation that incorporation was not increased when both enzymes were present. The major tryptic phosphopeptide obtained from tyrosine hydroxylase phosphorylated by each protein kinase exhibited an identical retention time following ...
TY - JOUR. T1 - A protein histidine kinase induced m rat liver by peroxisome proliferators. In vitro activation by Ras protein and guanine nucleotides. AU - Motojima, Kiyoto. AU - Goto, S.. PY - 1993/3/15. Y1 - 1993/3/15. N2 - A novel protein kinase is induced in rat liver plasma membrane by the administration of peroxisome proliferators. A 36 kDa protein (P36) on the membrane was rapidly phosphorylated in vitro by the kinase and the phosphorylated amino acid was identified as phosphohistidine. Histidine phosphorylation of P36 was activated in vitro by recombinant Ras protein and GTP; both decreased Michaelis constant (Km) for ATP from 1.25 to 0.25 μM. The novel histidine kinase, products of which have been overlooked due to their acid lability, may participate in cellular signaling and peroxisome proliferators may perturb the pathway.. AB - A novel protein kinase is induced in rat liver plasma membrane by the administration of peroxisome proliferators. A 36 kDa protein (P36) on the membrane ...
The induction of ornithine decarboxylase was studied following the stimulation of human peripheral blood lymphocytes with concanavalin A (ConA) (10 µg/ml). Following treatment with ConA, ornithine decarboxylase activity increased 4-5-fold between 6 and 12 hr of incubation and reached a peak level 10-12-fold above control (unstimulated) values by 48 hr. Increases in incorporation of [3H]uridine into acid-insoluble material followed a similar time course after the addition of ConA to lymphocytes. The rate of incorporation of [3H]thymidine into acid-insoluble material was maximal at 72 hr. The degree of activation of soluble cyclic 3,5-AMP-dependent protein kinase(s) was determined at various times following ConA stimulation. Between 1 and 2 hr after mitogen administration, the cyclic AMP-dependent protein kinase activity ratio increased markedly and was 0.23 unit above control values by 4 hr. The activity ratio decreased between 4 and 8 hr and returned to higher values after incubation with the ...
Trans-activation of the DNA-damage signalling protein kinase Chk2 by T-loop exchange The protein kinase Chk2 (checkpoint kinase 2) is a major effector of the replication checkpoint. Chk2 activation is initiated by phosphorylation of Thr68, in the serine glutamine/threonine-glutamine cluster domain (SCD), by ATM. The phosphorylated SCD-segment binds to the FHA domain of a second Chk2 molecule, promoting dimerisation of the protein and triggering phosphorylation of the activation segment/T-loop in the kinase domain. We have now determined the structure of the kinase domain of human Chk2 in complexes with ADP and a small-molecule inhibitor debromohymenialdisine. The structure reveals a remarkable dimeric arrangement in which T-loops are exchanged between protomers, to form an active kinase conformation in trans. Biochemical data suggest that this dimer is the biologically active state promoted by ATM-phosphorylation, and also suggests a mechanism for dimerisation-driven activation of Chk2 by ...
cAMP-dependent protein kinase complex, cytoplasm, nucleus, cAMP-dependent protein kinase activity, mitochondrion organization, protein kinase A signaling, protein phosphorylation, Ras protein signal transduction
Protein Kinase Substrate (PKS) Peptide Microarray - Comprehensive Service from LC Sciences,LC Sciences provides a comprehensive kinase analysis service utilizing high density protein kinase substrate (PKS) peptide microarrays synthesized on Paraflo microfluidic chips for proteomic scale kinase profiling, quantitative measurement of kinase kinetic activities, and drug discovery research.,biological,biology supply,biology supplies,biology product
A comparative analysis on protein kinases encoded in the completely sequenced genomes of two plant species, namely Arabidopsis thaliana and Oryza sativa spp japonica cv. Nipponbare is reported in the current study. We have analysed 836 and 1386 kinases identified from A. thaliana and the $O$. sativa genomes respectively. Their classification into known subfamilies reveals selective expansions of the plant receptor kinase subfamily comprising of Ser/Thr receptor kinases. The presence of calciumdependent kinases, and potential absence of cyclic nucleotide-dependent protein kinase of the type found in other (non-plant) eukaryotes, are other notable features of the two plant kinomes described here. An analysis on domain organisation of each of the protein kinases encoded in the plant genome has been carried out. Uncommon composition of functional domains like nuclear translocation factor domain, redox sensor domain (PAS), ACT and lectin domains are observed in few protein kinases shared between the ...
The activity of calcium-, phospholipid-dependent protein kinase (PKc) was measured in (a) total extracts, (b) crude membrane, and (c) cytosolic fractions of chick embryo myogenic cells differentiating in culture. Total PKc activity slowly declines during the course of terminal myogenesis in contrast to the activity of cAMP-dependent protein kinase, which was also measured in the same cells. Myogenic cells at day 1 of culture possess high particulate and low soluble PKc activity. A dramatic decline of particulate PKc activity occurs during myogenic cell differentiation and is accompanied, through day 4, by a striking rise of the soluble activity. The difference in the subcellular distribution of PKc between replicating myoblasts and myotubes is confirmed by phosphorylation studies conducted in intact cells. These studies demonstrate that four polypeptides whose phosphorylation is stimulated by the tumor promoter 12-O-tetradecanoyl phorbol 13-acetate in myotubes, are spontaneously phosphorylated ...
The RAC Beta Serine/Threonine Protein Kinase Market research report presents an all-inclusive study of the global RAC Beta Serine/Threonine Protein Kinase market. The report includes all the major trends and technologies performing a major role in the RAC Beta Serine/Threonine Protein Kinase market development during forecast period. The key players in the market are Almac Discovery Ltd, ArQule Inc, AstraZeneca Plc, Bayer AG, Critical Outcome Technologies Inc, Merck & Co Inc, Novartis AG. An attractiveness study has been presented for each geographic area in the report to provide a comprehensive analysis of the overall competitive scenario of the RAC Beta Serine/Threonine Protein Kinase market globally.. Apply here for the SAMPLE copy of the report @: Furthermore, the report comprises an outline of the diverse tactics used by the key players in the market. It also details the competitive scenario of the RAC Beta ...
In vitro phosphorylation of the regulatory subunit of yeast cAMP-dependent protein kinase was studied. The cAMP-binding regulatory subunit (R subunit) can be multiply phosphorylated. Three distinct phosphorylation sites were inferred from the different ATP concentrations required for phosphorylation and from the presence of two discrete mobility shifts in NaDodSO4/polyacrylamide gel electrophoresis of the R subunit on phosphorylation. Limited tryptic digestion of the phosphorylated R subunit showed that a Mr 37,000 cAMP-binding peptide contained one of the phosphorylation sites and that a separate Mr 12,000 peptide contained another phosphorylation site. The yeast R subunit is therefore similar to the type II R subunit of mammalian origin, although it has a larger Mr (64,000 vs. 58,000) and is multiply phosphorylated. In vivo, both phosphorylated and unphosphorylated forms of the R subunit were found in cells grown in lactate or to stationary phase in 1.5% glucose, while cells grown in 5% ...
The focus of this symposium was to present new information on the morphogenesis of Candida albicans, particularly how it relates to signal transduction pathways and other genes involved in the regulation of morphogenesis. In addition, we discuss the role of adherence and colonization of the oral cavity by the organism and discuss the role of mannan as an adhesin that recognizes the human red blood cell. C. albicans utilizes at least two signal pathways to regulate its conversion from a yeast form to filamentous growth (hyphae). One of these two pathways is similar to the Saccharomyces cerevisiae pseudohyphal/mating pathway, which utilizes the regulatory protein, Cphlp. The other pathway is not totally defined but requires a second regulatory protein, referred to as Efg1p. Other signal pathways may exist, which include a two-component histidine kinase and response regulator proteins. The latter pathway(s) may include proteins such as Chk1p, Ssk1p, Shi1p and Cos1p/Nik1p. Mutations in strains, which
cAMP-dependent protein kinases are reversibly complexed with any of the four isoforms of regulatory (R) subunits, which contain either a substrate or a pseudosubstrate autoinhibitory domain. The human protein kinase X (PrKX) is an exemption as it is inhibited only by pseudosubstrate inhibitors, i.e.
Price for Single User $ 3080 USD :: MAP Kinase Interacting Serine/Threonine Protein Kinase 1 (MAP Kinase Signal Integrating Kinase 1 or MKNK1 or EC - Pipeline Review, H2 2016SummaryGlobal Markets Directs, MAP Kinase Interacting Serine/Threonine Protein Kinase 1 (MAP Kinase
Regulatory subunit of the cyclic AMP-dependent protein kinase (PKA), an effector of the Ras/cAMP pathway. Inhibits PKA activity in the absence of cAMP. cAMP activates PKA and promotes growth and proliferation in response to good nutrient conditions. Together with ZDS1, provides a negative feedback control on the cell wall integrity-signaling pathway by acting as a negative regulator of MAP kinase SLT2/MPK1.
Mediates cAMP-dependent signaling triggered by receptor binding to GPCRs. PKA activation regulates diverse cellular processes such as cell proliferation, the cell cycle, differentiation and regulation of microtubule dynamics, chromatin condensation and decondensation, nuclear envelope disassembly and reassembly, as well as regulation of intracellular transport mechanisms and ion flux. Regulates the abundance of compartmentalized pools of its regulatory subunits through phosphorylation of PJA2 which binds and ubiquitinates these subunits, leading to their subsequent proteolysis ...
TY - JOUR. T1 - Synthesis and protein kinase C binding activity of benzolactam-V7. AU - Ma, Dawei. AU - Wang, Guoqiang. AU - Wang, Shaomeng. AU - Kozikowski, Alan P.. AU - Lewin, Nancy E.. AU - Blumberg, Peter M.. PY - 1999/5/17. Y1 - 1999/5/17. N2 - Benzolactam-V7 (3a), a simplified analogues of (-)-indolactam-V with twist-form conformation, was synthesized and evaluated as a new protein kinase C modulator. Both 3a and its-7-substituted analogue 3c showed weak binding activity to displace PDBU binding from recombinant PKCα.. AB - Benzolactam-V7 (3a), a simplified analogues of (-)-indolactam-V with twist-form conformation, was synthesized and evaluated as a new protein kinase C modulator. Both 3a and its-7-substituted analogue 3c showed weak binding activity to displace PDBU binding from recombinant PKCα.. UR - UR - U2 - ...
Cyclin-dependent kinases (Cdk) direct cell cycle transitions by associating with various cyclins throughout the cell cycle. For cells to exit mitosis, mitotic Cdk activity must be turned off. In Saccharomyces cerevisiae, the mitotic exit network, or MEN, comprises of a group of proteins that form a signaling pathway required for mitotic exit. The MEN regulates the activity of Cdc14, the protein phosphatase critical for inactivating mitotic Cdk. Components of the MEN include the protein kinases Cdc15 and Dbf2, as well as the Dbf2-associated protein Mob1. We determined how these proteins are organized within the MEN by determining the molecular mechanism of Dbf2 activation. Dbf2 requires Mob1 association in order to be active and Cdc15 phosphorylates and thereby activates the Dbf2-Mob1 protein kinase complex. We also determined that the conserved phosphorylation sites of the NDR protein kinase family are required for Dbf2 kinase activity in vitro as well as for DBF2 function in vivo. It is unknown ...
Two-component systems consisting of histidine kinases and their corresponding receivers are widespread in bacterial signal transduction. In the past few years, genes coding for homologues of two-component systems were also discovered in eukaryotic organisms. DokA, a homologue of bacterial histidine kinases, is an element of the osmoregulatory pathway in the amoeba Dictyostelium. The work described here addresses the question whether DokA is phosphorylated in vivo in response to osmotic stress. We have endogenously overexpressed individual domains of DokA to investigate post-translational modification of the protein in response to osmotic shock in vivo. Dictyostelium cells were labeled with [32P]-orthophosphate, exposed to osmotic stress and DokA fragments were subsequently isolated by immunoprecipitation. Thus, a stress-dependent phosphorylation could be demonstrated, with the site of phosphorylation being located in the kinase domain. We demonstrate biochemically that the phosphorylated amino acid is
Find Mitotic Checkpoint Serine/Threonine Protein Kinase (Bub) research area related information and Mitotic Checkpoint Serine/Threonine Protein Kinase (Bub) research products from R&D Systems. Learn more.
The mating response of the haploid yeast Saccharomyces cerevisiae provides a genetically tractable model system to study a G‐protein regulated mitogen‐activated protein (MAP) kinase cascade. This response is initiated by the pheromones a and α‐factor released from MATa and MATα cells, respectively. These short polypeptides bind to cell type‐specific receptors and thereby trigger the activation of a heterotrimeric G‐protein that is common to both cell types (for a review, see Herskowitz, 1995). The β and γ subunits of the G‐protein then activate a MAP kinase cascade consisting of Ste7p (a MAP kinase kinase or MEK homolog), Ste11p (a MEK kinase homolog) and the partially redundant MAP kinase homologs Fus3p and Kss1p (Herskowitz, 1995). The Ste20p protein kinase (a MEK kinase kinase) (Leberer et al., 1992a; Wu et al., 1995), Ste5p (Leberer et al., 1993; Whiteway et al., 1995) and Ste50p (Ramezani Rad et al., 1992) play crucial roles in the activation of this MAP kinase cascade which ...
Protein kinases play important roles in controlling biological functions. We employed PCR-based cloning technique to isolate a protein kinase gene from rice endosperm and obtained a novel protein kinase (REK) cDNA clone from a cDNA library constructed from maturing rice seed. The deduced amino acid …
These results indicate that the mechanism by which the US3 protein kinase blocks activation of the BAD protein does not depend on the phosphorylation of the regulatory serines or the interaction of BAD with the 14-3-3 proteins.. In an earlier article this laboratory reported that the US3 protein kinase blocked the apoptosis induced by the HSV-1 d120 mutant at a premitochondrial stage (21). Further studies revealed that the kinase also blocks programmed cell death induced by the proapoptotic protein BAD (22). In the studies reported here, we investigated the effects of the US3 protein kinase on the function and state of the BAD protein. We report several key findings below.. (i) In uninfected cells BAD was processed by at least two proteolytic cleavages that are blocked by caspase inhibitors. The untreated transduced cells expressed elevated caspase 3 activity.. (ii) In cells cotransduced with the US3 protein kinase, the BAD protein was not cleaved and the caspase 3 activity was not ...
[ 118 Pages| TOC | Tables | Figures] This report studies the MAP Kinase Interacting Serine Protein Kinase 1 market size (value and volume) by players, regions, product types and end industries, history data 2014-2018 and forecast data 20
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Decoding Ca2 Signals Through Plant Protein Kinases ----------------------------------------- DOWNLOAD: ----------------------------------------- Decoding Ca(2+) signals through plant protein kinases. Plants harbor four families of kinases that have been implicated in Ca(2+) signaling (CDPKs, CRKs, CCaMKs, and SnRK3s). . Some of the calcium-regulated kinases also show potential for regulation by lipid signals and kinase cascades. 10 Aug 2010 . Ca2+-binding proteins and protein kinases decode these complex Ca2+ fingerprints through conformational coupling and covalent modifications of proteins. . In plants, Ca2+-dependent protein kinases and Ca2+/calmodulin-dependent protein kinases are involved in decoding Ca2+ signals into phosphorylation signals. Differential innate immune signalling via Ca(2+) sensor protein kinases. Nature 464 . Decoding Ca(2+) signals through plant protein kinases. Annu. Rev. 5 Mar 2014 . of the CBLs/CIPKs complex in decoding Ca2+ signals, thereby . G.;
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The osmotic balance between the cytoplasmic and extracellular compartments of cells is critical for the control of cell volume. A mammalian protein kinase, Jnk, which is a distant relative of the mitogen-activated protein kinase group, was activated by phosphorylation on threonine and tyrosine in osmotically shocked cells. The activation of Jnk may be relevant to the biological response to osmotic shock because the expression of human Jnk in the yeast Saccharomyces cerevisiae rescued a defect in growth on hyper-osmolar media. These data indicate that related protein kinases may mediate osmosensing signal transduction in yeast and mammalian cells. ...
[51 Pages Report] Check for Discount on Cyclin-Dependent Kinase 1 (p34 Protein Kinase or Cell Division Protein Kinase 1 or CDK1 or EC - Pipeline Review, H1 2016 report by Global Markets Direct. Global Markets Directs, Cyclin-Dependent Kinase 1 (p34 Protein...
This chapter focuses on other modalities of signal transduction, including intracellular second messengers, feedback regulation, and posttranslational modifications such as the phosphorylation-dephosphorylation of proteins. Empirical studies of archaeal-archaeal and archaeal-bacterial communication have been few in number and preliminary in nature. Inspection of archaeal genomes has revealed them to be devoid of homologs of the prototypic bacterial quorum-sensing proteins LuxS and LuxR. Two-component systems differ in several fundamental respects from protein-serine/threonine/tyrosine phosphorylation cascades. First, autophosohorylation is the predominant mechanism of phosphorylation in the two-component system, whereas protein-serine/threonine/tyrosine phosphorylation cascades rely primarily on phosphotransfer reactions catalyzed by protein kinases that are distinct from the phosphoacceptor protein. Second, the chemical nature of the phosphoryl moieties formed during two-component signaling differs
The acronym CK2 (derived from the misnomer casein kinase 2) denotes one of the most pleiotropic members of the eukaryotic protein kinase superfamily, characterized by an acidic consensus sequence in which a carboxylic acid (or pre-phosphorylated) side chain at position n+3 relative to the target serine/threonine residue plays a crucial role. The latest repertoire of CK2 substrates includes approx. 300 proteins, but the analysis of available phosphopeptide databases from different sources suggests that CK2 alone may be responsible for the generation of a much larger proportion (10-20%) of the eukaryotic phosphoproteome. Although for the time being CK2 is not included among protein kinases whose inhibitors are in clinical practice or in advanced clinical trials, evidence is accumulating that elevated CK2 constitutive activity co-operates to induce a number of pathological conditions, including cancer, infectious diseases, neurodegeneration and cardiovascular pathologies. The development and ...
|p|GF 109203X is a potent and selective inhibitor of protein kinase C [1].|/p||p| Protein kinase C (PKC) is a family of protein kinase enzymes that are involved in controlling the function of other proteins through the phosphorylation of serine and threon
Figure 1 Insulin-stimulated mTOR protein kinase activity. 3T3-L1 adipocytes were incubated without insulin or with 10 milliunits/ml insulin for 30 min. Extracts were prepared and immunoprecipitations were performed with either nonimmune IgG (NI-IgG) or mTAb2. Beads were suspended in reaction mix containing [γ-32P]ATP and His6-PHAS-I, and then incubated for 30 min. After the reactions had been terminated, samples were subjected to SDS/PAGE and autoradiograms of the dried gels were prepared. (A) An autoradiogram showing 32P-labeled His6-PHAS-I (Left) and an immunoblot prepared with mTAb2 (Right) are presented. Other immunoprecipitations were performed as described above. (B) Prior to incubation in reaction mix, beads were incubated for 30 min at 22°C in buffer A alone or buffer A supplemented with 200 μg/ml GST-FKBP12 (FKBP) and 5 μM rapamycin. Buffer A contained 50 mM NaCl, 10 mM NaHepes, and 50 mM β-glycerophosphate (pH 7.4). The beads were then washed twice before incubation in reaction ...
In this short communication we report for the first time to our knowledge the use of ESTBlast to in silico clone a new gene and a step by step description of this particular in silico cloning project.
In the presence of DNA damage, the protein kinase Chk1 can effect cell cycle arrest. Chen et al. determined the crystal structure of the Chk1 kinase domain (Chk1KD), and have uncovered some of its regulatory mechanisms. In the presence or absence of the nonhydrolyzable analog AMP-PNP, no conformational change was observed in the Chk1KD ATP binding site, catalytic residues, or activation loop. Therefore, the conformation of Chk1KD approximates its activated ATP-bound state, and Chk1 does not appear to require activation loop phosphorylation before activity. The authors determined that the regulation of Chk1 may be controlled by its COOH-terminal region; the kinase activity of Chk1KD was 20 times that of full-length Chk1, and autophosphorylation of full-length Chk1 did not inherently affect its kinase activity. The authors speculate on the role of the COOH-terminus in autoinhibition. The crystal structure of the linker region between the kinase domain and the COOH-terminal region indicates that, ...
The gene IKKE produces a protein kinase also known as IKKE. Protein kinases are enzymes that turn other proteins on or off. The IKKE protein kinase appears to target proteins which, in turn, control genes that regulate the mouse metabolism.. When the high-fat diet is fed to a normal mouse, IKKE protein-kinase levels rise, the metabolic rate slows, and the animal gains weight. In that situation, the IKKE protein kinase acts as a brake on the metabolism. Knockout mice placed on the high-fat diet did not gain weight, apparently because deleting the IKKE gene releases the metabolic brake, allowing it to speed up and burn more calories, instead of storing those calories as fat.. The knockout mice are not exercising any more than the control mice used in the study. Theyre just burning more energy, Saltiel said. And in the process, theyre generating a little heat, as well - their body temperature actually increases a bit.. Saltiels team is now searching for small molecules that block IKKE ...
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RAC Gamma Serine/Threonine Protein Kinase Market Forecast To 2026 | Covid-19 Impact And Global Analysis By Type, Application, And End User
The Hybrid Histidine Kinase LadS Forms a Multicomponent Signal Transduction System with the GacS/GacA Two-Component System in Pseudomonas aeruginosa ...
Beta-1 adrenergic receptor, Beta-2 adrenergic receptor, Beta-3 adrenergic receptor, Mitogen-activated protein kinase 1, Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 3-kinase regulatory subunit beta, Phosphatidylinositol 3-kinase regulatory subunit gamma, CAMP ...
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Publications, Scientific Experts, Research Topics, Species, Genomes and Genes, Research Grants about cyclic gmp dependent protein kinases
Allende JE, Allende CC (1995). "Protein kinases. 4. Protein kinase CK2: an enzyme with multiple substrates and a puzzling ... "Characterization of protein interaction among subunits of protein kinase CKII in vivo and in vitro". Mol. Cells. 8 (1): 43-8. ... a novel pleckstrin homology domain-containing protein that interacts with protein kinase CK2". J. Biol. Chem. 275 (19): 14295- ... Faust M, Montenarh M (2001). "Subcellular localization of protein kinase CK2. A key to its function?". Cell Tissue Res. 301 (3 ...
The protein is also predicted to have a polo-box domain (PBD) of polo-like kinase 4 (plk4), which has predicted conservation in ... This analysis indicates C5orf34 as a phosphoprotein and supports structural predictions of it being a kinase protein. The ... The protein is serine and threonine rich. The charge distribution of the protein is equally dispersed per there are no positive ... provided a predicted human protein structure that indicated domains of plk polo-box of the serine/threonine-protein kinase plk4 ...
... , a Golgi localized protein kinase, is a serine kinase that phosphorylates both casein and other highly acidic proteins ... FAM20C is a secretory kinase, responsible for the phosphorylation of all secreted proteins, from milk to bone proteins. ... Tagliabracci VS, Pinna LA, Dixon JE (Mar 2013). "Secreted protein kinases". Trends in Biochemical Sciences. 38 (3): 121-30. doi ... "Secreted kinase phosphorylates extracellular proteins that regulate biomineralization". Science. 336 (6085): 1150-3. doi: ...
Protein kinase C activation[edit]. PIP2 cleavage to IP3 and DAG initiates intracellular calcium release and PKC activation. ... "Protein Kinase C as the Receptor for the Phorbol Ester Tumor Promoters: Sixth Rhoads Memorial Award Lecture". Cancer Research. ... whereas DAG is a physiological activator of protein kinase C (PKC). The production of DAG in the membrane facilitates ... Diacylglycerol can be phosphorylated to phosphatidic acid by diacylglycerol kinase. Insulin resistance[edit]. Activation of PKC ...
Hz2V110 is homologous to serine/threonine protein kinase (S_TPK). S_TPK catalyzes phosphorylation of serine and threonine ... Edelman AM, Blumenthal DK, Krebs EG (June 1987). "Protein serine/threonine kinases". Annual Review of Biochemistry. 56 (1): 567 ... "Choristoneura fumiferana Granulovirus p74 protein, a highly conserved baculoviral envelope protein". Journal of Biochemistry ... Of the 113 ORFs that are likely to encode proteins, 66 are on the forward strand of DNA, the other 47 on the reverse. All of ...
Phosphorylation by cAMP-dependent protein kinases[edit]. Cyclic AMP-dependent protein kinases (protein kinase A) are activated ... receptor domain by protein kinases. This process uncouples Gs protein from the LHCGR. Another way to desensitize is to uncouple ... G-protein coupled receptor signaling pathway. • male gonad development. • male genitalia development. • cognition. • G-protein ... G-protein coupled peptide receptor activity. • G-protein coupled receptor activity. • choriogonadotropin hormone binding. • ...
Lu demonstrated that glycolytic enzyme pyruvate kinase M2 (PKM2) acts as a protein kinase and phosphorylates histone H3 to ... "Metabolic Kinases Moonlighting as Protein Kinases". Trends in Biochemical Sciences. 43 (4): 301-310. doi:10.1016/j.tibs.2018.01 ... In addition to the findings that metabolic enzymes of PKM2, PGK1, KHK-A, and PCK1 can function as protein kinases, he ... fructose kinase KHK-A is highly expressed in hepatocellular carcinoma cells by alternate splicing and acts as a protein kinase ...
"Fluid shear stress activation of focal adhesion kinase. Linking to mitogen-activated protein kinases". J. Biol. Chem. 272 (48 ... Corbalan-Garcia S, Yang SS, Degenhardt KR, Bar-Sagi D (1996). "Identification of the mitogen-activated protein kinase ... nucleotide exchange protein Sos and a 75-kDa protein that is a substrate for T cell antigen receptor-activated tyrosine kinases ... Genetic analysis indicated that CDC25 is essential for activation of RAS proteins. In Drosophila, the protein encoded by the ' ...
There are 2 common types of CAM Kinase proteins: specialized and multi-functional CAM kinases. Substrate-specific CAM Kinases ... β CAMKIIδ CAMKIIγ CAMKIII CAMKIV CAMKV CaM kinase like vesicle associated SCAMK Ca2+/calmodulin-dependent protein kinase kinase ... This group of proteins includes CAMK III. More on CAMKIII can be found following this link. Multi-functional CAM Kinases have ... Taylor SS, Yang J, Wu J, Haste NM, Radzio-Andzelm E, Anand G (March 2004). "PKA: a portrait of protein kinase dynamics". ...
... calmodulin-modulated myosin light chain kinase; RAF/MEK/Mitogen-activated protein kinases; PKC/Ca2+/Calcineurin/Nuclear factor ... to activate the Rho family of GTPases signaling proteins and Gi-Gβγ G proteins to activateRaf/MEK/mitogen-activated kinase ... regulation of proliferation by activation of the epidermal growth factor receptor and mitogen-activated protein kinase ... phospholipase C/IP3/cell Ca2+ mobilization/diacylglycerol/protein kinase Cs; ...
Norbury C (1995). "Cdk2 protein kinase (vertebrates)". In Hardie DG, Hanks S (eds.). Protein kinase factsBook. Boston: Academic ... CDK interacting protein/Kinase inhibitory protein) family and the INK4a/ARF (Inhibitor of Kinase 4/Alternative Reading Frame) ... Nigg EA (June 1995). "Cyclin-dependent protein kinases: key regulators of the eukaryotic cell cycle". BioEssays. 17 (6): 471-80 ... Originally, a green fluorescent protein, mAG, was fused to hGem(1/110) and an orange fluorescent protein (mKO2) was fused to ...
... of antigen receptor induces Syk-dependent activation of p70S6 kinase through protein kinase C and phosphoinositol 3-kinase". ... Latour S, Veillette A (June 2001). "Proximal protein tyrosine kinases in immunoreceptor signaling". Current Opinion in ... Activatory motifs (ITAMs) bind kinases, such as Syk family kinases (e.g. ZAP70 for T-cell receptor) that phosphorylate a range ... If the kinase is associated with an NTR, aggregation brings two or more SFK into close proximity, which allows them to ...
The Src-family kinases are examples of proteins that utilize autophosphorylation to sustain their activated states. Src kinases ... Protein kinases, many of which are regulated by autophosphorylation, are vital in controlling the cellular proliferation, ... Jacobs MD, Caron PR, Hare BJ (Mar 2008). "Classifying protein kinase structures guides use of ligand-selectivity profiles to ... Wang J, Wu JW, Wang ZX (Dec 2011). "Structural insights into the autoactivation mechanism of p21-activated protein kinase". ...
Smith JA, Francis SH, Corbin JD (November 1993). "Autophosphorylation: a salient feature of protein kinases". Mol. Cell. ... Scaffold (disambiguation) Protein kinase Chemotherapy Thrombolysis Cancer research. ... PCI contains a small cysteine-rich module, called a T-knot scaffold, that is shared by several different protein families, ... a Lin SL, Nussinov R (October 1995). "A disulphide-reinforced structural scaffold shared by small proteins with diverse ...
... which is a part of the regulatory mechanism that enables the SR proteins to control RNA splicing. This protein kinase is ... "The Clk2 and Clk3 dual-specificity protein kinases regulate the intranuclear distribution of SR proteins and influence pre-mRNA ... Dual specificity protein kinase CLK2 is an enzyme that in humans is encoded by the CLK2 gene. This gene encodes a member of the ... Hanes J, von der Kammer H, Klaudiny J, Scheit KH (Dec 1994). "Characterization by cDNA cloning of two new human protein kinases ...
... protein tyrosine kinases and protein serine/threonine kinases. Dual-specificity kinases are subclass of the tyrosine kinases. ... PIKKs have four domains at the protein level, which distinguish them from other protein kinases. From the N-terminus to the C- ... mTOR is a kinase within the family of phosphatidylinositol-3 kinase-related kinases (PIKKs), which is a family of serine/ ... threonine protein kinases, with a sequence similarity to the family of lipid kinases, PI3Ks. These kinases have different ...
Hanks SK, Hunter T (May 1995). "Protein kinases 6. The eukaryotic protein kinase superfamily: kinase (catalytic) domain ... B-Raf is a member of the Raf kinase family of growth signal transduction protein kinases. This protein plays a role in ... while the protein is more formally known as serine/threonine-protein kinase B-Raf. The B-Raf protein is involved in sending ... Once B-Raf is activated, a conserved protein kinase catalytic core phosphorylates protein substrates by promoting the ...
"A family of human cdc2-related protein kinases." The EMBO Journal 11.8 (1992): 2909. Whyte, Peter, Nicola M. Williamson, and E ... Meyerson, M (1992). "A family of human cdc2-related protein kinases". EMBO J. 11: 2909-17. doi:10.1002/j.1460-2075.1992.tb05360 ... Among Harlow's discoveries was the demonstration that the retinoblastoma protein interacts with viral transforming proteins, ... "The retinoblastoma protein is phosphorylated during specific phases of the cell cycle." Cell 58.6 (1989): 1097-1105. van den ...
A-kinase anchor protein 5 is a protein that in humans is encoded by the AKAP5 gene. The A-kinase anchor proteins (AKAPs) are a ... 1995). "Association of protein kinase A and protein phosphatase 2B with a common anchoring protein". Science. 267 (5194): 108- ... "A-kinase anchoring protein 79/150 facilitates the phosphorylation of GABA(A) receptors by cAMP-dependent protein kinase via ... "Localization of the cAMP-dependent protein kinase to the postsynaptic densities by A-kinase anchoring proteins. ...
Serine/threonine-protein kinase 3 is an enzyme that in humans is encoded by the STK3 gene. Protein kinase activation is a ... The yeast 'sterile 20' (Ste20) kinase acts upstream of the mitogen-activated protein kinase (MAPK) cascade that is activated ... "Entrez Gene: STK3 serine/threonine kinase 3 (STE20 homolog, yeast)". "PhosphoSitePlus: Serine/threonine-protein kinase 3 - ... protein kinase B), blocking autophosphorylation of Thr180, MST2 cleavage, kinase activity, and translocation to the nucleus. In ...
A-kinase anchor protein 8 is an enzyme that, in humans, is encoded by the AKAP8 gene. The A-kinase anchor proteins (AKAPs) are ... Collas P, Le Guellec K, Taskén K (Dec 1999). "The A-kinase-anchoring protein AKAP95 is a multivalent protein with a key role in ... 2003). "Protein kinase A-anchoring protein AKAP95 interacts with MCM2, a regulator of DNA replication". J. Biol. Chem. 278 (29 ... Collas P, Le Guellec K, Taskén K (2000). "The A-kinase-anchoring protein AKAP95 is a multivalent protein with a key role in ...
CLK1 Phosphorylates serine/arginine-rich proteins involved in pre-mRNA processing in the nucleus. CDK16 (gene) A protein kinase ... Lipp JJ, Marvin MC, Shokat KM, Guthrie C (August 2015). "SR protein kinases promote splicing of nonconsensus introns". Nature ... "NCBI Protein". National Center for Biotechnology Information. "Protein Molecular Weight Calculator". ... "Synergistic Gene Expression Signature Observed in TK6 Cells upon Co-Exposure to UVC-Irradiation and Protein Kinase C-Activating ...
Yuan H, Marmorstein R (February 2013). "Histone acetyltransferases: Rising ancient counterparts to protein kinases". ... structural proteins, polyamines, and proteins involved in nuclear import. Acetylation of these proteins can alter their ability ... Histones comprise the protein portion of chromatin. There are five different histone proteins: H1, H2A, H2B, H3, and H4. A core ... In addition, since contacts between CoA and protein facilitate the formation of favorable histone-protein contacts, it is ...
"The Fes protein-tyrosine kinase phosphorylates a subset of macrophage proteins that are involved in cell adhesion and cell-cell ... Tyrosine-protein kinase Fes/Fps also known as proto-oncogene c-Fes/Fps is an enzyme that in humans is encoded by the FES gene. ... Overview of all the structural information available in the PDB for UniProt: P07332 (Tyrosine-protein kinase Fes/Fps) at the ... The gene product has tyrosine-specific protein kinase activity and that activity is required for maintenance of cellular ...
Fan G, Shumay E, Wang H, Malbon CC (2001). "The scaffold protein gravin (cAMP-dependent protein kinase-anchoring protein 250) ... Piontek J, Brandt R (2003). "Differential and regulated binding of cAMP-dependent protein kinase and protein kinase C ... "The scaffold protein gravin (cAMP-dependent protein kinase-anchoring protein 250) binds the beta 2-adrenergic receptor via the ... A-kinase anchor protein 12, aka AKAP250, is an enzyme that in humans is encoded by the AKAP12 gene. The A-kinase anchor ...
The protein encoded by this gene belongs to the cdc2/cdkx subfamily of the ser/thr family of protein kinases. It may play a ... "Entrez Gene: PCTK1 PCTAIRE protein kinase 1". Cheng K, Li Z, Fu WY, Wang JH, Fu AK, Ip NY (Aug 2002). "Pctaire1 interacts with ... Serine/threonine-protein kinase PCTAIRE-1 is an enzyme that in humans is encoded by the PCTK1 gene. ... Graeser R, Gannon J, Poon RY, Dubois T, Aitken A, Hunt T (2002). "Regulation of the CDK-related protein kinase PCTAIRE-1 and ...
... by agents that activate other protein kinases such as mitogen-activated protein kinase (p38 MAP kinase). Heterologous ... This commonly occurs with G protein coupled receptors (see Protein kinase C#Function); cytokine and other non-G protein couple ... It commonly occurs with G protein-coupled receptors where it is mediated by the G protein-coupled receptor kinases (GRK) and ... However, some stimuli cause cells to activate protein kinase Cs that act to desensitize multiple types of receptors thereby ...
... strong interest has shifted towards the aurora kinase proteins. The kinase gene Aurora A when amplified acts as an oncogene ... Mayor T, Meraldi P, Stierhof YD, Nigg EA, Fry AM (June 1999). "Protein kinases in control of the centrosome cycle". FEBS ... The activated GTP-bound form of Ran releases microtubule-stabilizing proteins, such as TPX2, from protein complexes in the ... but the protein Aurora B (a kinase conserved from yeast to vertebrates) detects and eliminates this type of anchoring. (Note: ...
A-kinase anchor protein 6 is an enzyme that in humans is encoded by the AKAP6 gene. The A-kinase anchor proteins (AKAPs) are a ... "Cloning and characterization of A-kinase anchor protein 100 (AKAP100). A protein that targets A-kinase to the sarcoplasmic ... "Entrez Gene: AKAP6 A kinase (PRKA) anchor protein 6". Marx, S O; Reiken S; Hisamatsu Y; Jayaraman T; Burkhoff D; Rosemblit N; ... Kapiloff MS, Schillace RV, Westphal AM, Scott JD (1999). "mAKAP: an A-kinase anchoring protein targeted to the nuclear membrane ...
Shiloh Y (March 2003). "ATM and related protein kinases: safeguarding genome integrity". Nature Reviews. Cancer. 3 (3): 155-68 ... The proteins expressed by the hMre11 (defective in ATLD) and Nbs1 (defective in NBS) genes exist in the cell as a complex, ... Thus, the similarity of the three diseases can be explained in part by the fact that the protein products of the three genes ... This risk is probably a secondary effect of their immunodeficiency and not a direct effect of the lack of ATM protein. The most ...
1985). "Amino terminal myristylation of the protein kinase p60src, a retroviral transforming protein". Science. 227 (4685): 427 ... 1990). "Myristoylation of gag proteins of HIV-1 plays an important role in virus assembly". AIDS Res. Hum. Retroviruses. 6 (6 ... Tashiro A, Shoji S, Kubota Y (1990). "Antimyristoylation of the gag proteins in the human immunodeficiency virus-infected cells ... Zhou W, Resh MD (1997). "Differential membrane binding of the human immunodeficiency virus type 1 matrix protein". J. Virol. 70 ...
ER Translocon complex.[2] Many protein complexes are involved in protein synthesis. The actual production takes place in the ... Sec61 is the protein-conducting channel and the OST adds sugar moieties to the nascent protein. ... Oligosaccharyltransferase or OST (EC is a membrane protein complex that transfers a 14-sugar oligosaccharide from ... Yeast OST is composed of eight different membrane-spanning proteins in three subcomplexes (one of them is OST4).[7][8] These ...
Kumar S, Sieghart W, Morrow AL (2002). "Association of protein kinase C with GABA(A) receptors containing alpha1 and alpha4 ... This membrane protein-related article is a stub. You can help Wikipedia by expanding it.. *v ... Gamma-aminobutyric acid receptor subunit alpha-4 is a protein that in humans is encoded by the GABRA4 gene.[5][6] ... GABRA4+protein,+human at the US National Library of Medicine Medical Subject Headings (MeSH) ...
A protein kinase drifting around on the outer chloroplast membrane can use ATP to add a phosphate group to the Toc34 protein, ... It can be regulated through phosphorylation, but by a different protein kinase than the one that phosphorylates Toc34.[41] Its ... Protein targeting and importEdit. See also: Protein targeting. The movement of so many chloroplast genes to the nucleus means ... Protein synthesisEdit. See also: Transcription and translation. Protein synthesis within chloroplasts relies on an RNA ...
The CD20 proteins are sticking out of the cell membrane, and rituximab, the Y-shaped antibody, is binding to the CD20 proteins. ... Tyrosine-kinase inhibitors ("-nib"). Receptor tyrosine kinase. *ErbB: HER1/EGFR (Brigatinib. *Erlotinib ... The antibody binds to the cell surface protein CD20. CD20 is widely expressed on B cells, from early pre-B cells to later in ... In contrast, when the B cell lacked this asymmetric protein cluster, it was killed only 40% of the time.[36][37] ...
negative regulation of protein kinase activity. • cytokine-mediated signaling pathway. • negative regulation of JAK-STAT ... protein kinase inhibitor activity. • collagen binding. • extracellular matrix structural constituent conferring compression ... a newly discovered member of the leucine-rich repeat protein family". The Journal of Biological Chemistry. 276 (15): 12212-21. ... a novel member of the leucine-rich repeat protein family closely related to decorin and biglycan". The Journal of Biological ...
"The neuropeptide substance P activates p38 mitogen-activated protein kinase resulting in IL-6 expression independently from NF- ... "Metalloproteinases and transforming growth factor-alpha mediate substance P-induced mitogen-activated protein kinase activation ... "Substance P induces rapid and transient membrane blebbing in U373MG cells in a p21-activated kinase-dependent manner". PLOS ... "Inhibitor of apoptosis proteins (IAPs) and their antagonists regulate spontaneous and tumor necrosis factor (TNF)-induced ...
Like lapatinib and neratinib, afatinib is a protein kinase inhibitor that also irreversibly inhibits human epidermal growth ... Binding proteins: IGFBP (1, 2, 3, 4, 5, 6, 7). *Cleavage products/derivatives with unknown target: Glypromate (GPE, (1-3)IGF-1) ... Phase II results for breast cancer that over-expresses the protein human epidermal growth factor receptor 2 (Her2-positive ... Afatinib is not only active against EGFR mutations targeted by first generation tyrosine-kinase inhibitors (TKIs) like ...
Mijelin protein nula • Osteonektin • Protein C • Protein S • Proteoglikan • Serum amiloid P komponenta • Sialoglikoprotein ( ... and c-Jun NH2-terminal kinase.". J. Biol. Chem. 274 (23): 15978-81. PMID 10347144. doi:10.1074/jbc.274.23.15978. CS1 održavanje ... Faktor aktivacije B-ćelija, (BAFF) koji je takođe poznat kao faktor nekroze tumora ligand superfamilija član 13B, je protein ... On je izražen kao transmembranski protein na različitim ćelijskim tipovima, kao što su monociti, dendritske ćelije i ćelije ...
Vallenius T، Mäkelä TP (2003). "Clik1: a novel kinase targeted to actin stress fibers by the CLP-36 PDZ-LIM protein.". J. Cell ... "Towards a proteome-scale map of the human protein-protein interaction network.". Nature. 437 (7062): 1173-8. PMID 16189514. doi ... Wang H، Harrison-Shostak DC، Lemasters JJ، Herman B (1996). "Cloning of a rat cDNA encoding a novel LIM domain protein with ... Vallenius T، Luukko K، Mäkelä TP (2000). "CLP-36 PDZ-LIM protein associates with nonmuscle alpha-actinin-1 and alpha-actinin-4 ...
... quercetin is a non-specific protein kinase enzyme inhibitor.[17][20] Quercetin has also been reported to have estrogenic ( ... Quercetin also activates or inhibits the activities of a number of proteins.[22] For example, ... quercetin has also been found to act as an agonist of the G protein-coupled estrogen receptor (GPER).[26][27] ... "The G protein-coupled receptor GPR30 mediates c-fos up-regulation by 17beta-estradiol and phytoestrogens in breast cancer cells ...
... mitogen-activated protein kinase) cascade that is itself a kinase. RSK2 phosphorylates cellular proteins (including histone H3 ... Mutations in the RPS6KA3 gene can result in expression of an RSK2 protein (ribosomal S6 kinase 2) with reduced or absent kinase ... The protein RSK2 which is encoded by the RPS6KA3 gene is a kinase which phosphorylates some substrates like CREB and histone H3 ... Mutations in the RPS6KA3 disturb the function of the protein, but it is unclear how a lack of this protein causes the signs and ...
protein binding. • enzyme binding. • receptor binding. • lipid binding. • RNA polymerase II transcription factor activity, ... In vitro phosphorylation by casein kinase II". The Journal of Biological Chemistry. 269 (49): 31034-40. PMID 7983041.. ... The progesterone receptor (PR), also known as NR3C3 or nuclear receptor subfamily 3, group C, member 3, is a protein found ... identical protein binding. • RNA polymerase II transcription factor activity, sequence-specific DNA binding. • transcriptional ...
The encoded protein is a type 1A regulatory subunit of protein kinase A. Inactivating germline mutations of this gene are found ... transition in the second codon position of the 74th codon in the protein) mutation in the PRKAR1A gene confirming the diagnosis ...
Fig 2. Schematic diagram of a GABAA receptor protein ((α1)2(β2)2(γ2)) which illustrates the five combined subunits that form ... Bcr-Abl tyrosine-kinase inhibitors. *Cannabinoid receptor antagonists. *CCR5 receptor antagonists. *Neurokinin 1 receptor ... The synaptic anchoring protein Gephyrin is indirectly linked to the GABAA receptors. ... molecules that increase the activity of the GABAA receptor protein in the vertebrate central nervous system. ...
... binding to cAMP-dependent protein kinase (PKA).[111] Moclobemide is chemically unrelated to irreversible MAOI antidepressants ... The elimination half-life is around 2 hours.[8][118] It is moderately bound to plasma proteins, especially albumin.[8] However ...
Adducin binds with high affinity to Ca(2+)/calmodulin and is a substrate for protein kinases A and C. Alternative splicing ... Matsuoka Y, Li X, Bennett V (1998). "Adducin is an in vivo substrate for protein kinase C: phosphorylation in the MARCKS- ... Definition of the calmodulin-binding domain and sites of phosphorylation by protein kinases A and C". J. Biol. Chem. 271 (41): ... Alpha-adducin is a protein that in humans is encoded by the ADD1 gene. Adducins are a family of cytoskeleton proteins encoded ...
positive regulation of protein kinase activity. • T cell activation involved in immune response. • cellular protein metabolic ... protein processing. • protein maturation. • myeloid dendritic cell differentiation. • autophagy. • protein glycosylation. • ... negative regulation of protein kinase activity. • cell fate specification. • skeletal system morphogenesis. • regulation of ... positive regulation of protein phosphorylation. • positive regulation of MAP kinase activity. • positive regulation of ...
The active site is a region on an enzyme which a particular protein or substrate can bind to. The active site will only allow ... "Functional Design of Proteins". Molecular Cell Biology. 4th edition. W. H. Freeman. ...
protein C-terminus binding. • protein binding. • four-way junction DNA binding. • identical protein binding. • ... Lin HR, Ting NS, Qin J, Lee WH (Sep 2003). "M phase-specific phosphorylation of BRCA2 by Polo-like kinase 1 correlates with the ... This protein can interact with the ssDNA-binding protein RPA, BRCA2, PALB2[10] and RAD52. ... Protein domains in homologous recombination-related proteins are conserved across the three main groups of life: archaea, ...
"Human tyrosine kinase 2 deficiency reveals its requisite roles in multiple cytokine signals involved in innate and acquired ... Genetic disorder, protein biosynthesis: Transcription factor/coregulator deficiencies. (1) Basic domains. 1.2. *Feingold ...
1992). "The lymphocyte-specific tyrosine protein kinase p56lck is endocytosed in Jurkat cells stimulated via CD2.". J. Immunol. ... to the transmembrane protein GP41 of HIV-1 inhibits distinct lymphocyte activation pathways dependent on protein kinase C and ... Wilkins A, Yang W, Yang J (2003). "Structural biology of the cell adhesion protein CD2: from molecular recognition to protein ... 1990). "Immunoregulatory effect of a synthetic peptide corresponding to a region of protein p24 of HIV.". Folia Biol. (Praha) ...
Perets T, Blumenstein Y, Shistik E, Lotan I, Dascal N (Apr 1996). "A potential site of functional modulation by protein kinase ... Calcium channel, voltage-dependent, L type, alpha 1C subunit (also known as Cav1.2) is a protein that in humans is encoded by ... Click on genes, proteins and metabolites below to link to respective Wikipedia articles. [§ 1] ... protein binding. • alpha-actinin binding. • voltage-gated calcium channel activity. • voltage-gated calcium channel activity ...
TANGO6: encoding protein Transport and Golgi organization protein 6 homolog. *TAO2: encoding Serine/threonine-protein kinase ... UNKL: encoding protein RING finger protein unkempt-like. *VAT1L: encoding protein Vesicle amine transport protein 1 homolog (T ... LINC00273 encoding protein Long intergenic non-protein coding RNA 273. *LOC124220: encoding protein Zymogen granule protein 16 ... SHCBP1: encoding protein SHC SH2 domain-binding protein 1. *SLZ1: encoding protein SLX1 structure-specific endonuclease subunit ...
"The Drosophila Clock Gene double-time Encodes a Protein Closely Related to Human Casein Kinase Iε" (PDF). Cell. 94 (1): 97-107 ... In 1998, Jeff Price from the Young lab discovered a kinase called doubletime(Casein kinase 1) that phosphorylates PER on ... Young's lab is also attributed with the discovery of the timeless and doubletime genes, which makes proteins that are also ... Period and Timeless proteins bind together to form a stabilized dimer, which allows the two to enter the nucleus. ...
... who believed that transcription was activated by protein-DNA and protein-protein interactions on largely naked DNA templates, ... The mitotic kinase aurora B phosphorylates histone H3 at serine 10, triggering a cascade of changes that mediate mitotic ... Nuclear protein Ataxia-Telangiectasia (NPAT), also known as nuclear protein coactivator of histone transcription, is a ... The first step of chromatin structure duplication is the synthesis of histone proteins: H1, H2A, H2B, H3, H4. These proteins ...
This bacterial protein complex is a machine for folding other proteins, which get trapped within the shell. Fatty acid synthase ... Arias-Palomo E, Recuero-Checa MA, Bustelo XR, Llorca O (December 2007). "3D structure of Syk kinase determined by single- ... Proteins in vitreous ice usually adopt a random distribution of orientations (or viewing angles), allowing a fairly isotropic ... Important information on protein synthesis, ligand binding and RNA interaction can be obtained using this novel technique at ...
Kelly CJ, Stenton SR, Lashen H. Insulin-like growth factor binding protein-1 in PCOS: a systematic review and meta-analysis. ... of 17α-Hydroxylase Activity Is Mediated by Phosphatidyl Inositol 3-Kinase But Not Extracellular Signal-Regulated Kinase-1/2 in ...
Cyclin-T2 is a protein that in humans is encoded by the CCNT2 gene. The protein encoded by this gene belongs to the highly ... This cyclin and its kinase partner CDK9 were found to be subunits of the transcription elongation factor p-TEFb. The p-TEFb ... Kwak YT, Ivanov D, Guo J, Nee E, Gaynor RB (1999). "Role of the human and murine cyclin T proteins in regulating HIV-1 tat- ... Jang MK, Mochizuki K, Zhou M, Jeong HS, Brady JN, Ozato K (2005). "The bromodomain protein Brd4 is a positive regulatory ...
... and two kinases of the JNK MAP kinase pathway (MLK2 and MKK7). He then determined that CNK1 acts together with these four ... It was already known that other Ga proteins could induce Rho activation (i.e. Ga13 activates p115 Rho GEF, which in turn ... In 1993, Alan Hall was awarded the Feldberg Foundation Prize for his work on the role GTP-binding proteins played on signal ... In 1986, Hall helped uncover properties of the human p21 protein, which is encoded by N-ras. GTPase activity of different ...
Signals through Kit receptor tyrosine kinase are essential for development of erythrocytes, melanocytes, germ cells, mast cells ... Signals through Kit receptor tyrosine kinase are essential for development of erythrocytes, melanocytes, germ cells, mast cells ...
MAP kinase kinase kinase (MAP3K or MKKK). *MAP kinase kinase kinases *MAP3K1 ... A mitogen-activated protein kinase (MAPK or MAP kinase) is a type of protein kinase that is specific to the amino acids serine ... Dephospho-(reductase kinase) kinase (EC *AMP-activated protein kinase α *PRKAA1 ... is performed by members of the Ste7 protein kinase family, also known as MAP2 kinases. MAP2 kinases in turn, are also activated ...
... protein kinases are implicated in a broad variety of diseases, including cancers and neurodegenerative conditions, and offer ... Assays for Mitogen-Activated Protein Kinase (MARK) Subtypes and MARK Activating Protein Kinase-2 (MAPKAP K-2) Using a Common ... Analysis of Protein Kinase Subcellular Localization by Visualization of GFP Fusion Proteins ... In Protein Kinase Protocols, a panel of highly skilled laboratory investigators describe both basic and more sophisticated ...
Protein kinase C (PKC). is actually a family of protein kinases consisting of ~10 isozymes. They are divided into three ... Dephospho-(reductase kinase) kinase (EC *AMP-activated protein kinase α *PRKAA1 ... A serine/threonine protein kinase (EC is a kinase enzyme that phosphorylates the OH group of serine or threonine ( ... Protein Kinase B, also known as AKT kinase. The v-akt gene was identified as the oncogene of retrovirus AKT8. The gene codes ...
... John C. Watson jcwatso at Tue Dec 30 12:32:19 EST 1997 *Previous message: Postdoctoral ... POSTDOCTORAL POSITION AT IUPUI A postdoctoral position is available to study photoregulated protein kinases from the garden pea ... Expression of the two kinases under investigation is rapidly down-regulated by light. One kinase is closely related to the blue ... Genetic, molecular, and biochemical approaches will be utilized to elucidate the roles of these kinases in the transduction of ...
Mitogen-activated protein kinases in innate immunity.. Arthur JS1, Ley SC. ... the extracellular signal-regulated kinase (ERK), p38 and Jun N-terminal kinase (JNK) subfamilies. In conjunction with the ... surface and in the cytoplasm of innate immune cells activates members of each of the major mitogen-activated protein kinase ( ... Mitogen-Activated Protein Kinases/antagonists & inhibitors. *Mitogen-Activated Protein Kinases/immunology*. *Toll-Like ...
... providing a high level of internal dynamics of the protein kinase. During the course of evolution, protein kinases developed a ... EPKs are represented by Protein kinase A (panel B). Structural elements conserved in all kinases are shown as white (N-lobe) ... Protein kinases: evolution of dynamic regulatory proteins.. Taylor SS1, Kornev AP. ... do not form sequential motifs coming from different parts of protein kinases sequence. A. Four residues from 25 human kinases ...
We combine protein signatures from a number of member databases into a single searchable resource, capitalising on their ... InterPro provides functional analysis of proteins by classifying them into families and predicting domains and important sites ... Bifunctional protein HldE. Shewanella loihica (strain ATCC BAA-1088 / PV-4). Loading... ... Bifunctional protein HldE. Shewanella putrefaciens (strain CN-32 / ATCC BAA-453). Loading... ...
Activation of cyclin A-dependent protein kinases during apoptosis. W Meikrantz, S Gisselbrecht, S W Tam, and R Schlegel ... activation of cyclin A-dependent protein kinases, is also an important event during apoptosis. ... Proteins in the blood of mice may underlie the cognition-enhancing properties of young blood. ... to 7-fold increases in cyclin A-associated histone H1 kinase activity, levels approximating the mitotic value. Where examined, ...
We combine protein signatures from a number of member databases into a single searchable resource, capitalising on their ... InterPro provides functional analysis of proteins by classifying them into families and predicting domains and important sites ... Protein kinase C zeta plays a central role in activation of the p42/44 mitogen-activated protein kinase by endotoxin in ... This group represents protein kinase C (KPC), including zeta/iota types from mammals, protein kinase C-like 3 from round worms ...
At a 1X concentration this reaction buffer assures optimal activity of protein kinases, including Abl Protein Tyrosine Kinase ( ... Abl), CDK1-cyclin B, CaMKII, p42 MAP Kinase (MAPK). ... Casein Kinase II (CK2) * cAMP-dependent Protein Kinase (PKA), ... At a 1X concentration this reaction buffer assures optimal activity of protein kinases, including Abl Protein Tyrosine Kinase ( ... At a 1X concentration the NEBuffer for Protein Kinases (PK) assures optimal activity of protein kinase enzymes. ...
... cyclic AMP-dependent protein kinase, and calcium/calmodulin-dependent protein kinase. For two of these kinases (cyclic AMP- and ... Protein kinase C. Bipolar disorders. Drugs for bipolars. Lithium prophylaxis. The manic spectrum. Schizoaffective disorder. The ... The protein kinase C cascade. Mania: lithium versus divaplroex. Dysthymia, hyperthymia and cyclothymia. Refs. and further ... Second messenger-regulated protein kinases in the brain: their functional role and the action of antidepressant drugs by. ...
... and methods of using them to treat tyrosine kinase-dependent diseases and conditions in mammals: wherein n is an integer, ... regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, ... Protein tyrosine kinase inhibitors. US20090298855 *. Jul 28, 2009. Dec 3, 2009. Critical Outcome Technologies Inc.. Protein ... The FLK family is comprised of the kinase insert domain receptor (KDR), fetal liver kinase-1 (FLK-1), fetal liver kinase-4 (FLK ...
AMP-activated protein kinase (AMPK), an energy sensor, can regulate protein and lipid metabolism responding to alterations in ...
An easy-to-use directory for life science and biomedical research products. Find special deals on products, order catalogs and browse product lines from suppliers of reagents, antibodies, laboratory equipment, and more.
Protein kinases such as Cyclin-dependent kinase 5 (Cdk5) and c-Jun N-terminal kinases (JNKs) involve these steps. In this ... Protein kinases such as Cyclin-dependent kinase 5 (Cdk5) and c-Jun N-terminal kinases (JNKs) involve these steps. In this ... Migrating neurons also have intrinsic machineries to regulate cytoskeletal proteins and adhesion properties. Protein ... Migrating neurons also have intrinsic machineries to regulate cytoskeletal proteins and adhesion properties. Protein ...
... including the tumor suppressor protein p53, the SV40 large T antigen and several transcription factors. ... DNA-Dependent Protein Kinase (DNA-PK) phosphorylates several DNA-binding substrates in vitro, ... cAMP-Dependent Protein Kinase, Catalytic Subunit. Purified kinase for protein phosphorylation and signal transduction studies. ... Kinase-Glo® Luminescent Kinase Assays. Determines activity of purified kinases by quantifying ATP remaining after a kinase ...
Engineering allosteric regulation in protein kinases. By David Pincus, Jai P. Pandey, Zoë A. Feder, Pau Creixell, Orna Resnekov ... Engineering allosteric regulation in protein kinases. By David Pincus, Jai P. Pandey, Zoë A. Feder, Pau Creixell, Orna Resnekov ... Engineering allosteric regulation in protein kinases Message Subject. (Your Name) has forwarded a page to you from Science ...
Emerging evidence demonstrates that some metabolic enzymes, such as pyruvate kinase M2 (PKM2), phosphoglycerate kinase 1 (PGK1 ... Protein kinases regulate every aspect of cellular activity, whereas metabolic enzymes are responsible for energy production and ... Metabolic Kinases Moonlighting as Protein Kinases Trends Biochem Sci. 2018 Apr;43(4):301-310. doi: 10.1016/j.tibs.2018.01.006. ... and nucleoside diphosphate kinase 1 and 2 (NME1/2), that phosphorylate soluble metabolites can also function as protein kinases ...
The mitogen-activated protein kinases (MAP kinases) p42mapk and p44mapk are serine/threonine kinases rapidly activated in cells ... Mitogen-activated protein kinases p42mapk and p44mapk are required for fibroblast proliferation. G Pagès, P Lenormand, G ... Mitogen-activated protein kinases p42mapk and p44mapk are required for fibroblast proliferation ... Mitogen-activated protein kinases p42mapk and p44mapk are required for fibroblast proliferation ...
protein kinase C, eta type. A. 157. Homo sapiens. Mutation(s): 0 Gene Names: PRKCH, PKCL, PRKCL. EC: (PDB Primary Data ... Protein kinase C eta (PKCeta) is one of several PKC isoforms found in humans. It is a novel PKC isoform in that it is activated ... Protein kinase C eta (PKCeta) is one of several PKC isoforms found in humans. It is a novel PKC isoform in that it is activated ... Structure of human protein kinase C eta (PKCeta) C2 domain and identification of phosphorylation sites.. Littler, D.R., Walker ...
Bovine Proteins. Bovine Albumin Bovine Transferrin CellMaxx Thrombin >> View All Bovine Proteins Empowered. Amino Acids and ... Proteins, Enzymes & Peptides*Molecular Biology Enzymes*PCR Enzymes/Kits*Taq DNA Polymerase*with Standard Buffer ... Bovine Albumin Bovine Transferrin CellMaxx Thrombin >> View All Bovine Proteins Food & Biodiesel Analysis. Platforms, Analyzers ... FastDNA™ Isolation Kits FastRNA™ Isolation Kits FastProtein™ Isolation Kits >> View All DNA™, RNA™ & Protein™ Kits Purification ...
Regulation of Protein Kinases that Control Cell Growth Lead researcher. Professor B E Kemp, Mr C M House ...
View protein in PROSITE. PS00107 PROTEIN_KINASE_ATP, 1 hit. PS50011 PROTEIN_KINASE_DOM, 1 hit. PS00109 PROTEIN_KINASE_TYR, 1 ... View protein in PROSITE. PS00107 PROTEIN_KINASE_ATP, 1 hit. PS50011 PROTEIN_KINASE_DOM, 1 hit. PS00109 PROTEIN_KINASE_TYR, 1 ... IPR011009 Kinase-like_dom_sf. IPR000719 Prot_kinase_dom. IPR017441 Protein_kinase_ATP_BS. IPR001245 Ser-Thr/Tyr_kinase_cat_dom ... IPR011009 Kinase-like_dom_sf. IPR000719 Prot_kinase_dom. IPR017441 Protein_kinase_ATP_BS. IPR001245 Ser-Thr/Tyr_kinase_cat_dom ...
View protein in InterPro. IPR011009 Kinase-like_dom_sf. IPR003527 MAP_kinase_CS. IPR000719 Prot_kinase_dom. ... View protein in InterPro. IPR011009 Kinase-like_dom_sf. IPR003527 MAP_kinase_CS. IPR000719 Prot_kinase_dom. ... Kinase, Serine/threonine-protein kinaseSAAS annotation. Automatic assertion according to rulesi ... PROSITE; a protein domain and family database. More...PROSITEi. View protein in PROSITE. PS01351 MAPK, 1 hit. PS50011 PROTEIN_ ...
... is a highly specific substrate for DNA-PK, with the sequence Glu-Pro-Pro-Leu-Ser ... DNA-Dependent Protein Kinase. Purified kinase that phosphorylates several DNA-binding proteins in vitro, including p53. ... DNA-Dependent Protein Kinase. Purified kinase that phosphorylates several DNA-binding proteins in vitro, including p53. ... cAMP-Dependent Protein Kinase, Catalytic Subunit. Purified kinase for protein phosphorylation and signal transduction studies. ...
... is a truncated form of the v-AbI Protein Tyrosine Kinase, a partner in the Gag-Abl fusion protein of the Abelson murine ... 1X NEBuffer™ for Protein Kinases (PK) Incubate at 30°C 1X NEBuffer™ for Protein Kinases (PK) 50 mM Tris-HCl 10 mM MgCl2 0.1 mM ... Abl Protein Tyrosine Kinase (AbI) is a truncated form of the v-AbI Protein Tyrosine Kinase, a partner in the Gag-Abl fusion ... NEBuffer™ for Protein Kinases (PK) -20 10 X Product Categories:. Discontinued Products. * Properties & Usage Unit Definition. ...
Eukayotic protein kinases evolved as a family of highly dynamic molecules with strictly organized internal architecture. A ... providing a high level of internal dynamics of the protein kinase. During the course of evolution, protein kinases developed a ... Protein kinases: evolution of dynamic regulatory proteins Trends Biochem Sci. 2011 Feb;36(2):65-77. doi: 10.1016/j.tibs.2010.09 ... Protein kinases thus represent a unique, highly dynamic, and precisely regulated set of switches that control most biological ...
Protein Kinase A is directed to specific sub cellular locations after tethering to Protein kinase A anchoring proteins (AKAPs ... out of 540 different protein kinase genes that make up for human kinome, only one other protein kinase, Casein kinase 2, is ... "cAMP-dependent protein kinase" redirects here. It is not to be confused with AMP-activated protein kinase or cyclin-dependent ... Protein kinase A, more precisely known as adenosine 3,5-monophosphate (cyclic AMP)-dependent protein kinase was discovered by ...
... Halyna M. Kuznietsova, Maryna S. Yena, Iryna P. Kotlyar ... In our previous studies we showed antitumor and anti-inflammatory activities of protein kinases inhibitor pyrrol derivate 1-(4- ... Increase of malonic dialdehyde (MDA) by 89% and protein carbonyl groups (PCG) by 60% and decrease of superoxide dismutase (SOD ...
  • This tandem activation loop phosphorylation (that was proposed to be either distributive or processive, dependent on cellular environment) is performed by members of the Ste7 protein kinase family, also known as MAP2 kinases . (
  • MAP2 kinases in turn, are also activated by phosphorylation, by a number of different upstream serine-threonine kinases ( MAP3 kinases ). (
  • Protein phosphorylation in particular plays a significant role in a wide range of cellular processes and is a very important posttranslational modification . (
  • For some of the various signaling pathways affected by antidepressant treatment, it was shown that protein phosphorylation, which represents an obligate step for most pathways, is markedly affected by long-term treatment. (
  • Antidepressant treatment activates the two kinases and increases the endogenous phosphorylation of selected substrates (microtubule-associated protein 2 and synaptotagmin). (
  • The changes in protein phosphorylation induced by long-term antidepressant treatment may contribute to explain the therapeutic action of antidepressants and suggest new strategies of pharmacological intervention. (
  • Extracellular cues such as Reelin induce intracellular signaling cascades through the protein phosphorylation. (
  • Protein phosphorylation regulates these processes. (
  • The mitogen-activated protein kinases (MAP kinases) p42mapk and p44mapk are serine/threonine kinases rapidly activated in cells stimulated with various extracellular signals by dual phosphorylation of tyrosine and threonine residues. (
  • The recognition motif for phosphorylation by Abl is I/V/L Y XXP/F. Abl, like many cytosolic protein tyrosine kinases, preferentially phosphorylates sites recognized by its own SH2 domain, selects substrates with large hydrophobic amino acids at the +3 position and β-branched amino acids at the -1 position (4). (
  • They won the Nobel Prize in Physiology or Medicine in 1992 for their work on phosphorylation and dephosphorylation and how it relates to protein kinase A activity. (
  • A group of enzymes that are dependent on cyclic GMP and catalyzes the phosphorylation of serine or threonine residues of proteins. (
  • MKK3 and SEK activate p38 MAP kinase by phosphorylation at Thr-180 and Tyr-182. (
  • A protein kinase is a kinase which selectively modifies other proteins by covalently adding phosphates to them (phosphorylation) as opposed to kinases which modify lipids, carbohydrates, or other molecules. (
  • Phosphorylation usually results in a functional change of the target protein (substrate) by changing enzyme activity, cellular location, or association with other proteins. (
  • Kinases are turned on or off by phosphorylation (sometimes by the kinase itself - cis-phosphorylation/autophosphorylation), by binding of activator proteins or inhibitor proteins, or small molecules, or by controlling their location in the cell relative to their substrates. (
  • While MAP kinases are serine/threonine-specific, they are activated by combined phosphorylation on serine/threonine and tyrosine residues. (
  • Protein kinases are enzymes that add a phosphate group to a protein or other organic molecule (phosphorylation). (
  • Phosphorylation usually alters the functional characteristics of the target protein and can act as an on/off switch for protein functions. (
  • A protein kinase activator enhances phosphorylation. (
  • Protein phosphorylation is one of the most important molecular mechanisms by which extracellular signals produce their biological responses in cells. (
  • Protein kinases (PKs) are key components of protein phosphorylation based signaling networks in eukaryotic cells. (
  • This provides a starting point for comprehensive analysis of protein phosphorylation in normal and disease states, as well as a detailed view of the current state of human genome analysis through a focus on one large gene family. (
  • Ever since the discovery nearly 50 years ago that reversible phosphorylation regulates the activity of glycogen phosphorylase, there has been intense interest in the role of protein phosphorylation in regulating protein function. (
  • Protein phosphorylation also plays a critical role in intercellular communication during development, in physiological responses and in homeostasis, and in the functioning of the nervous and immune systems. (
  • Mitochondrial deoxyguanosine kinase (DGUOK) is required for the phosphorylation of several deoxyribonucleosides and certain purine deoxykribonucleoside analogs widely employed as antiviral and chemotherapeutic agents. (
  • In mammalian cells, the phosphorylation of purine deoxyribonucleosides is mediated predominantly by 2 deoxyribonucleoside kinases: cytosolic deoxycytidine kinase (DCK) and mitochondrial deoxyguanosine kinase (DGUOK also known as DGK). (
  • 1991) "Protein Kinase C Substrate and Inhibitor Characteristics of Peptides Derived From the Myristoylated Alanine-Rich C Kinase Substrate (MARCKS) Protein Phosphorylation Site Domain" The Journal of Biological Chemistry266(22):14390-14398. (
  • The invention provides a method for determining an amino acid sequence motif for a phosphorylation site of a protein kinase. (
  • The invention also provides peptide substrates for protein kinase A, cell cycle control kinases, src family kinases, the EGF receptor and p92.sup.c-fps/fes based upon amino acid sequence motifs for the phosphorylation sites of these kinases. (
  • 1.1 A Brief History of Protein Phosphorylation. (
  • This induces the activation and nuclear accumulation of the kinase and the phosphorylation of diverse substrates, thus eliciting appropriate cellular responses. (
  • Numerous studies in non-neuronal tissues have shown that this transport mechanism is reversibly regulated by phosphorylation/dephosphorylation of the catalytic α subunit and/or associated proteins. (
  • Phosphorylation by the protein kinases PKG and PKC inhibits NKA activity, whereas dephosphorylation by the protein phosphatases PP-1 and PP-2B (calcineurin) reverses this effect. (
  • We have found that neuronal NKA activity is oppositely regulated by phosphorylation and dephosphorylation, and we have identified the main protein kinases and phosphatases mediating this regulation. (
  • Example neurons, phosphorylation of protein kinases, peptide hormones, and rod cells in the eyes. (
  • Our standard content PKS peptide microarray includes a comprehensive list of kinases and their related experimentally verified Serine, Threonine, and Tyrosine phosphorylation sites compiled from the Phospho.ELM database. (
  • We observed surprisingly high sequence coverage on some proteins, enabling further analyses of phosphorylation sites for several target kinases without additional sample processing. (
  • A dynamic transverse enrichment of atypical protein kinase C (aPKC) shifts the balance and transiently targets activated small GTPase RhoA , myosin phosphorylation and Rab11 vesicle trafficking to longitudinal junctions. (
  • Activity of the atypical protein kinase C (aPKC) is a key output of the Par complex as phosphorylation removes substrates from the Par domain. (
  • Each protein contains a basic and hydrophobic (BH) motif that interacts directly with phospholipids and also overlaps with aPKC phosphorylation sites. (
  • A protein kinase is a kinase enzyme that modifies other proteins by chemically adding phosphate groups to them (phosphorylation). (
  • As a result, protein kinase inhibitors are important research tools to study cell functions and human diseases. (
  • ARTICLE{Davies00specificityand, author = {Stephen P. Davies and Helen Reddy and Matilde Caivano and Philip Cohen}, title = {Specificity and mechanism of action of some commonly used protein kinase inhibitors}, journal = {Biochem. (
  • The specificities of 28 commercially available compounds reported to be relatively selective inhibitors of particular serine� threonine-specific protein kinases have been examined against a large panel of protein kinases. (
  • Ro 318220 and related bisindoylmaleimides, as well as H89, HA1077 and Y 27632, were more selective inhibitors, but still inhibited two or more protein kinases with similar potency. (
  • His current research focuses on the exploration of cellular signaling pathways in cell lines with respect to the role of various protein kinases using newly characterized kinase inhibitors identified by screening small chemical compound libraries. (
  • Protein kinase C inhibitors, H-7 or sphingosine, restored the abnormal acetylcholine-induced relaxations as well as suppressed the abnormal release of prostanoids in aorta exposed to elevated glucose. (
  • 1976) "Synthetic Hexapeptide Substrates and Inhibitors of 3':5'-Cyclic AMP-Dependent Protein Kinase" Proc. (
  • Burke, T. R. (1992) "Protein-Tyrosine Kinase Inhibitors" Drugs Fut. (
  • Thetext also describes existing and emerging kinase inhibitors,focusing mostly on small molecules but also alternative approacheslike therapeutic antibodies. (
  • We describe a streamlined mass spectrometry-based chemoproteomics workflow to examine the SAR and target profiles of a small library of kinase inhibitors that consists of the drug dasatinib and a panel of general type II inhibitors. (
  • Whereas the first mode of inhibition is mediated by JAK's own pseudokinase domain as well as the action of phosphatases, the second is achieved by the action of the SOCS (suppressor of cytokine signalling) proteins, negative-feedback inhibitors of JAK-mediated signalling. (
  • however, drugs that target RTKs, known as tyrosine kinase inhibitors (TKIs) have not been effective in treating breast cancer. (
  • Because MAP2 kinases display very little activity on substrates other than their cognate MAPK, classical MAPK pathways form multi-tiered, but relatively linear pathways. (
  • Thus, the two substrates of this enzyme are ATP and a protein , whereas its two products are ADP and phosphoprotein . (
  • While serine/threonine kinases all phosphorylate serine or threonine residues in their substrates, they select specific residues to phosphorylate on the basis of residues that flank the phosphoacceptor site, which together comprise the consensus sequence . (
  • While the catalytic domain of these kinases is highly conserved , the sequence variation that is observed in the kinome (the subset of genes in the genome that encode kinases) provides for recognition of distinct substrates. (
  • ELKs (panels A and C) contain multiple non-conserved helices that accommodate non-peptide substrates and are specific for each kinase. (
  • His research is focused on the identification and characterization of new substrates of protein kinase CK2 from Saccharomyces cerevisiae. (
  • 1990) "Identification of Major Nucleolar Proteins As Candidate Mitotic Substrates of cdc2 Kinase" Cell 60:791-801. (
  • In the method of the invention, a protein kinase is contacted with an oriented degenerate peptide library, peptides within the library which are substrates for the kinase are converted to phosphopeptides and the phosphopeptides are separated from non-phosphorylated peptides. (
  • The present invention relates to compounds of the Formula I, the pharmaceutically acceptable salts and stereoisomers thereof, which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent. (
  • Up to 30% of all human proteins may be modified by kinase activity, and kinases are known to regulate the majority of cellular pathways, especially those involved in signal transduction. (
  • Tyrosine-specific protein kinases (EC and EC phosphorylate tyrosine amino acid residues, and like serine/threonine-specific kinases are used in signal transduction. (
  • MAPKs belong to an evolutionarily conserved and ubiquitous signal transduction superfamily of Ser/Thr protein kinases that regulate multiple cellular processes including apoptosis, growth, differentiation and responses to environmental stimuli. (
  • The activators of p38 (MKK3 and MKK6), JNK (MKK4 and MKK7), and ERK (MEK1 and MEK2) define independent MAP kinase signal transduction pathways. (
  • Protein kinases are intimately integrated in different signal transduction pathways for the regulation of cardiac function in both health and disease. (
  • Such opposing effects of each signal transduction pathway seem to depend upon the duration and intensity of stimulus as well as the type of kinase isoform for each kinase. (
  • Signal transduction- the interaction of ligand and receptor proteins initiates this process, which converts the information in the signal into a cellular response. (
  • Since the consensus sequence residues of a target substrate only make contact with several key amino acids within the catalytic cleft of the kinase (usually through hydrophobic forces and ionic bonds ), a kinase is usually not specific to a single substrate, but instead can phosphorylate a whole "substrate family" which share common recognition sequences. (
  • Most kinases are inhibited by a pseudosubstrate that binds to the kinase like a real substrate but lacks the amino acid to be phosphorylated. (
  • Once released from their inhibitory Regulatory subunit, the catalytic subunits can go on to phosphorylate a huge number of other proteins in the minimal substrate context Arg-Arg-X-Ser/Thr. (
  • Two C-terminal cyclic nucleotide binding (CNB) domains cooperatively bind two molecules of cAMP, resulting in a conformational change of the R subunit that releases the active catalytic kinase subunit(s) from the inhibitory pseudo-substrate or substrate site of PKAR. (
  • We will not only review the well-known members of the family, such as kinase suppressor of Ras (KSR), but also put a special focus on the function of the recently identified or less studied scaffolders, such as fibroblast growth factor receptor substrate 2, flotillin-1 and mitogen-activated protein kinase organizer 1. (
  • LC Sciences provides a comprehensive kinase analysis service utilizing high density protein kinase substrate (PKS) peptide microarrays synthesized on Paraflo microfluidic chips for proteomic scale kinase profiling, quantitative measurement of kinase kinetic activities, and drug discovery research. (
  • This study shows that Par3 conserved region 3 (CR3) forms a tight inhibitory complex with a primed aPKC kinase domain, blocking substrate access. (
  • The developmental expression and the cellular localization of neurogranin (formerly designated p17), a brain-specific protein kinase C (PKC) substrate, were investigated. (
  • In comparison to the three-tiered classical MAPK pathways, some atypical MAP kinases appear to have a more ancient, two-tiered system. (
  • As key components of many cell signaling pathways, protein kinases are implicated in a broad variety of diseases, including cancers and neurodegenerative conditions, and offer considerable potential as tractable targets for therapeutic intervention. (
  • In the 20 years since Paul Simpson initially demonstrated that neurohormonal stimulation of cultured neonatal cardiomyocytes results in cellular hypertrophy, characteristic changes in cardiac gene expression, and activation of specific kinase signaling pathways ( 1 - 3 ), protein kinases have attracted attention as candidate mediators of the cardiac biomechanical stress and trophic responses. (
  • We demonstrate that mitogen-activated protein kinase pathways mediate inflammatory lung injury during ventilator-induced lung injury. (
  • Recent research has focused on intracellular signaling pathways involved in the development of VILI, among which include the mitogen-activated protein kinase (MAPK) pathways, key regulators of inflammation [7] - [9] . (
  • Stress-activated protein kinase (SAPK) pathways are conserved MAPK signaling modules that promote stress adaptation in all eukaryotic cells, including pathogenic fungi. (
  • and it is apparent that stress-activated protein kinase (SAPK) pathways are central in mediating such responses and virulence in many fungal pathogens. (
  • Given that these kinases and phosphatases serve as downstream effectors in key neuronal signaling pathways, they may mediate the coupling of primary messengers, such as neurotransmitters, hormones, and growth factors, to the NKAs, through which multiple brain functions can be regulated or dysregulated. (
  • Kinases regulate most cellular pathways and are responsible for the modification of nearly a third of all human proteins. (
  • Aberrant regulation of cell growth pathways is required for normal cells to become cancerous, and in many types of cancer, cell growth is driven by a group of enzymes known as receptor tyrosine kinases (RTKs). (
  • A mitogen-activated protein kinase ( MAPK or MAP kinase ) is a type of protein kinase that is specific to the amino acids serine and threonine (i.e., a serine/threonine-specific protein kinase ). (
  • MAPKs belong to the CMGC (CDK/MAPK/GSK3/CLK) kinase group. (
  • Following pathogen infection or tissue damage, the stimulation of pattern recognition receptors on the cell surface and in the cytoplasm of innate immune cells activates members of each of the major mitogen-activated protein kinase (MAPK) subfamilies--the extracellular signal-regulated kinase (ERK), p38 and Jun N-terminal kinase (JNK) subfamilies. (
  • At a 1X concentration this reaction buffer assures optimal activity of protein kinases, including Abl Protein Tyrosine Kinase (Abl) (NEB# P6050), CDK1-cyclin B (NEB# P6020), CaMKII (NEB #P6060), p42 MAP Kinase (MAPK) (NEB# P6080). (
  • p38 MAP Kinase (MAPK), also called RK or CSBP (Cytokinin Specific Binding Protein), is the mammalian orthologue of the yeast Hog1p MAP kinase, which participates in a signaling cascade controlling cellular responses to cytokines and stress. (
  • The MAPK superfamily includes three primary signaling cascades: the extracellular signal regulated kinases (ERK1/2), the c-Jun NH 2 -terminal kinases (JNK) and the p38 MAPKs. (
  • Mitogen-activated protein kinase kinase (also known as MAP2K , MEK , MAPKK ) is a kinase enzyme which phosphorylates mitogen-activated protein kinase (MAPK). (
  • Protein kinase A (PKA), Ca 2 + -calmodulin-dependent protein kinase (CaMK), protein kinase C (PKC), phosphoinositide 3-kinase (PI3K) and mitogen-activated protein kinase (MAPK) are not only involved in the control of subcellular activities for maintaining cardiac function, but also participate in the development of cardiac dysfunction in cardiac hypertrophy, diabetic cardiomyopathy, myocardial infarction, and heart failure. (
  • The mitogen-activated protein kinase (MAPK) pathway is the canonical signaling pathway for many receptor tyrosine kinases, such as the Epidermal Growth Factor Receptor. (
  • In recent years, it has become evident that MAPK signaling is regulated and fine-tuned by proteins that can bind to several MAPK signaling proteins simultaneously and, thereby, affect their function. (
  • These so-called MAPK scaffolding proteins are, thus, important coordinators of the signaling response in cells. (
  • In this review, we summarize the recent advances in the research on MAPK/extracellular signal-regulated kinase (ERK) pathway scaffolders. (
  • Any of a group of kinases that phosphorylate the amino acids serine, threonine, and tyrosine in certain proteins, that regulate essential aspects of cell growth and movement, and that can cause cancer and other diseases when dysfunctional. (
  • Activated p38 MAP kinase has been shown to phosphorylate and activate MAPKAP kinase 2 and to phosphorylate the transcription factors ATF2, Mac and MEF2. (
  • There are two main types of protein kinase, the great majority are serine/threonine kinases, which phosphorylate the hydroxyl groups of serines and threonines in their targets and the other are tyrosine kinases, although additional types exist. (
  • There are also protein kinases that phosphorylate other amino acids, including histidine kinases that phosphorylate histidine residues. (
  • Serine/threonine protein kinases (EC phosphorylate the OH group of serine or threonine (which have similar side-chains). (
  • The protein kinase family is large and important, but it is only one family in a larger superfamily of homologous kinases that phosphorylate a. (
  • Purdue University researchers have developed a high-throughput method for matching kinases to the proteins they phosphorylate, speeding the ability to identify multiple potential cancer drug targets. (
  • For example, receptor kinases in plants phosphorylate Ser and Thr residues, whereas in animals, the predominant type of receptor kinase phosphorylates Tyr residues. (
  • This is conducted by specialized enzymes of the STE protein kinase group. (
  • In enzymology , the term non-specific serine/threonine protein kinase describes a class of enzymes that belong to the family of transferases , specifically protein-serine/threonine kinases . (
  • These enzymes transfer phosphates to the oxygen atom of a serine or threonine sidechain in proteins . (
  • At a 1X concentration the NEBuffer for Protein Kinases (PK) assures optimal activity of protein kinase enzymes. (
  • Protein kinases regulate every aspect of cellular activity, whereas metabolic enzymes are responsible for energy production and catabolic and anabolic processes. (
  • The elevated protein kinase functions of these moonlighting metabolic enzymes in tumor development make them promising therapeutic targets for cancer. (
  • In cell biology , protein kinase A ( PKA [N 1] ) is a family of enzymes whose activity is dependent on cellular levels of cyclic AMP (cAMP). (
  • Eukaryotic protein kinases are enzymes that belong to a very extensive family of proteins that share a conserved catalytic core. (
  • Mutations and dysregulation of protein kinases play causal roles in human disease, affording the possibility of developing agonists and antagonists of these enzymes for use in disease therapy ( 7-9 ). (
  • Current Cancer Drug Targets aims to cover all the latest and outstanding developments on the medicinal chemistry, pharmacology, molecular biology, genomics and biochemistry of contemporary molecular drug targets involved in cancer, e.g. disease specific proteins, receptors, enzymes, genes. (
  • We provide unique one-stop products and services for assays of DNA, RNA, protein, enzymes, antibodies, or small molecules, as well as proven microfluidic technology and novel microarray chemistry for design of your miniaturized assay devices for diagnostics and biosensing applications. (
  • Drug compounds being developed at Purdue University could effectively target and inhibit protein kinase enzymes and secondary mutated versions that drive multiple types of cancers. (
  • In addition, plants contain a large group of kinases related to the classical SNF1-type kinases from yeast, although the majority of these enzymes in Arabidopsis have a different primary structure compared with their yeast homologs. (
  • Signals through Kit receptor tyrosine kinase are essential for development of erythrocytes, melanocytes, germ cells, mast cells and interstitial cells of Cajal (ICCs). (
  • Types include those acting directly as receptors ( Receptor protein serine/threonine kinase ) and Intracellular signaling peptides and proteins . (
  • Extracellular hormones such as glucagon and epinephrine begin an intracellular signalling cascade that triggers protein kinase A activation by first binding to a G protein-coupled receptor (GPCR) on the target cell. (
  • When a GPCR is activated by its extracellular ligand, a conformational change is induced in the receptor that is transmitted to an attached intracellular heterotrimeric G protein complex by protein domain dynamics . (
  • These kinases consist of a transmembrane receptor with a tyrosine kinase domain protruding into the cytoplasm. (
  • More than 50 receptor tyrosine kinases are known in mammals. (
  • A member of the death associated protein kinase (DAPk) family, DAPk1, has been implicated in cerebral ischemic damage, whereby DAPk1 potentiates NMDA receptor-mediated excitotoxicity through interaction with the NR2BR subunit. (
  • When the epidermal growth factor receptor (EGFR) on the cell's membrane is activated by a growth factor, the PKM2 protein moves into the cell nucleus, where it binds to the promoter regions of genes. (
  • Indicated in combination with capecitabine for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress the human epidermal receptor type 2 (HER2) protein and who have received prior therapy including an anthracycline, a taxane, and trastuzuma. (
  • ALW-II-41-27 is a novel Eph receptor tyrosine kinase inhibitor. (
  • A possible relationship between protein kinase C activation and impaired receptor-mediated endothelium-dependent relaxation in diabetes mellitus was examined in isolated aorta from normal rabbit exposed to elevated glucose. (
  • These findings suggest that the dysfunction of receptor-mediated endothelium-dependent relaxation associated with exposure to elevated glucose is due to increased production of vasoconstrictor prostanoids by the endothelium as a consequence of protein kinase C activation. (
  • 2.1 Ligand Binding to Receptor Tyrosine Kinases. (
  • This collection explores up-to-date descriptions of known G protein-coupled receptor kinase (GRK)-dependent mechanisms, both associated with G protein-coupled receptor (GPCR) functions and the receptor-independent. (
  • Authoritative and timely, G Protein-Coupled Receptor Kinases features the kind of comprehensive mechanistic elucidation of GRK functions and their regulation in cells necessary for a better understanding of cell biology as well as for devising novel research approaches and therapeutic strategies. (
  • pronounced "sarc", as it is short for sarcoma), is a non-receptor tyrosine kinase protein that in humans is encoded by the SRC gene. (
  • c-Src can be activated by many transmembrane proteins that include: adhesion receptors, receptor tyrosine kinases, G-protein coupled receptors and cytokine receptors. (
  • Most studies have looked at the receptor tyrosine kinases and examples of these are platelet derived growth factor receptor (PDGFR) pathway and epidermal growth factor receptor (EGFR). (
  • out of 540 different protein kinase genes that make up for human kinome, only one other protein kinase, Casein kinase 2 , is known to exist in a physiological tetrameric complex. (
  • The human genome contains about 500 protein kinase genes and they constitute about 2% of all human genes. (
  • A metabolic protein that nourishes cancer cells also activates tumor-promoting genes by loosening part of the packaging that entwines DNA to make up chromosomes, a team led by scientists at The University of Texas MD Anderson Cancer Center reports in the Aug. 16 issue of Cell . (
  • This separates another protein called histone deacetylase 3 (HDAC3) from the promoter regions of the genes CCND1 and MYC. (
  • HuSH-29 Kinase Collection contains 512 genes cloned in pRFP-C-RS vector allowing researchers to monitor transfection. (
  • We identify 518 putative protein kinase genes, of which 71 have not previously been reported or described as kinases, and we extend or correct the protein sequences of 56 more kinases. (
  • Chromosomal mapping revealed several small clusters of kinase genes and revealed that 244 kinases map to disease loci or cancer amplicons. (
  • Protein kinases are among the largest families of genes in eukaryotes ( 2-6 ) and have been intensively studied. (
  • A complete catalog of human protein kinases will aid in the discovery of human disease genes and in the development of therapeutics. (
  • The mutation or dysregulation of genes encoding protein kinases has been linked to many disease states, including diabetes, inflammatory disorders, and cancer. (
  • The eukaryotic protein kinase family is one of the largest gene families in all eukaryotes, counting for 2-4% of all genes. (
  • The Arabidopsis genome encodes 1,085 typical protein kinases (M. Gribskov, unpublished data), which is about 4% of the predicted 25,500 genes ( Arabidopsis Genome Initiative, 2000 ). (
  • In our previous studies we showed antitumor and anti-inflammatory activities of protein kinases inhibitor pyrrol derivate 1-(4-Cl-benzyl)-3-Cl-4-(CF3-fenylamino)-1H-pyrrol-2,5-dione (MI-1) on rat colon cancer model. (
  • Protein kinase inhibitor pyrrol derivate 1-(4-Cl-benzyl)-3-Cl-4-(CF 3 -fenylamino)-1Н-pyrrol-2,5-dione (MI-1) (Figure 1 ) has been synthesized at Chemistry Department of Taras Shevchenko National University of Kyiv. (
  • Genistein, a general kinase inhibitor, may be a potential antiviral for arenaviral hemorrhagic fever. (
  • Molecular Dynamics of Protein Kinase-Inhibitor Complexes: A Valid. (
  • Ponatinib is indicated for the treatment of adult patients with chronic phase, accelerated phase, or blast phase chronic myeloid leukemia (CML) that is resistant or intolerant to prior tyrosine kinase inhibitor therapy or Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ALL) that is resistant or intolerant to prior tyrosine kinase inhibitor therapy. (
  • Tafinlar is a kinase inhibitor that was initially indicated as a single agent for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E mutation as detected by an FDA-approved test [FDA label]. (
  • Ceritinib is a kinase inhibitor indicated for the treatment of patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) who have progressed on or are intolerant to crizotinib. (
  • 1986) "A Potent Synthetic Peptide Inhibitor of the cAMP-Dependent Protein Kinase" The Journal of Biological Chemistry261(3):989-992. (
  • 1985) "An Active Twenty-Amino-Acid-Residue Peptide Derived From the Inhibitor Protein of the Cyclic AMP-Dependent Protein Kinase" Biochem J. 231:655-661. (
  • 1.5 Comparison of Kinase Inhibitor Therapeutic Strategies. (
  • The ability to determine structure-activity relationships (SAR) and identify cellular targets from cell lysates and tissues is of great utility for kinase inhibitor drug discovery. (
  • Stringent selection criteria for target identification were applied to deduce 28 protein targets for dasatinib and 31 protein targets for our general type II kinase inhibitor in HeLa cell lysate. (
  • Additional kinase and protein targets were identified with the general type II inhibitor analogs, with small structural changes leading to divergent target profiles. (
  • Our rapid workflow profiled cellular targets for six small molecules within a week, demonstrating that an unbiased proteomics screen of cellular targets yields valuable SAR information and may be incorporated at an early stage in kinase inhibitor development. (
  • Serine/Threonine Kinase receptors play a role in the regulation of cell proliferation, programmed cell death ( apoptosis ), cell differentiation, and embryonic development. (
  • For all of the apoptosis-inducing agents tested, the appearance of condensed chromatin was accompanied by 2- to 7-fold increases in cyclin A-associated histone H1 kinase activity, levels approximating the mitotic value. (
  • These findings suggest that at least one of the biochemical steps required for mitosis, activation of cyclin A-dependent protein kinases, is also an important event during apoptosis. (
  • p38 mitogen-activated protein kinases are a class of mitogen-activated protein kinases (MAPKs) that are responsive to stress stimuli, such as cytokines, ultraviolet irradiation, heat shock, and osmotic shock, and are involved in cell differentiation, apoptosis and autophagy. (
  • Two major factors influence activity of MAP kinases: a) signals that activate transmembrane receptors (either natural ligands or crosslinking agents) and proteins associated with them (mutations that simulate active state) b) signals that inactivate the phosphatases that restrict a given MAP kinase. (
  • Various kinases are downstream effectors of neurohormone receptors that transduce signals from the sympathetic nervous and renin-angiotensin-aldosterone systems. (
  • The P38 MAP kinases are regulated by CYTOKINE RECEPTORS and can be activated in response to bacterial pathogens. (
  • C-type lectin receptors activate protein kinase C δ in a Syk-dependent manner to stimulate NF-κB signaling in response to fungi. (
  • We have thousands of products ranging from neuropeptides and hormones, to receptors, cytokines and growth factors , and kinases . (
  • Downstream of the receptors, this pathway involves the activation of a kinase cascade that culminates in a transcriptional response and affects processes, such as cell migration and adhesion. (
  • Due to their substantial involvement in signaling within and between cells, protein kinases have become the second most widely studied group of potential drug targets, after G-protein-coupled receptors (GPCR). (
  • G-protein coupled receptors (GPCR) are prominent targets in drug discovery. (
  • Protein kinase C iota type (PRKCI) is a calcium- and diacylglycerol-independent serine/ threonine-protein kinase that plays a general protective role against apoptotic stimuli, is involved in NF-kappa-B activation, cell survival, differentiation and polarity, and contributes to the regulation of microtubule dynamics in the early secretory pathway [ PMID: 10467349 , PMID: 11544035 , PMID: 11257119 ]. (
  • In the unphosphorylated structure both serines line the putative lipid-binding site and may therefore play a role in the lipid-regulation of the kinase. (
  • Protein kinase A has several functions in the cell, including regulation of glycogen , sugar , and lipid metabolism . (
  • Protein kinase A (PKA), the main effector of cAMP in eukaryotes, is a paradigm for the mechanisms of ligand-dependent and allosteric regulation in signalling. (
  • 7500 members that confers ligand-dependent allosteric regulation to a diverse range of proteins 2 . (
  • This book provides an overview of different protein kinases structure, function, regulation, and their role in cancer. (
  • 2.4 Protein Kinase Regulation. (
  • 2.4.4 Regulation by Other Domains and Partner Proteins. (
  • c-Src should not be confused with CSK (C-terminal Src kinase), an enzyme that phosphorylates c-Src at its C-terminus and provides negative regulation of Src's enzymatic activity. (
  • Broad in its range of techniques and thoroughly detailed to help ensure experimental success, Protein Kinase Protocols offers both novice and experienced investigators powerful tools for understanding the functional roles of specific protein kinases within signaling cascades and for identification and evaluation of novel therapeutic targets. (
  • Here we review recent developments in the area of these cardiotrophic kinases, highlighting the utility of animal models that are helping to identify molecular targets in the human condition. (
  • In view of the fact that most of these kinases are activated in heart disease and their inhibition has been shown to improve cardiac function, it is suggested that these kinases form excellent targets for drug development for therapy of heart disease. (
  • The compounds KT 5720, Rottlerin and quercetin were found to inhibit many protein kinases, sometimes much more potently than their presumed targets, and conclusions drawn from their use in cell-based experiments are likely to be erroneous. (
  • Protein kinases are key focus targets in drug discovery. (
  • cAMP-dependent protein kinase" redirects here. (
  • PKA is also known as cAMP-dependent protein kinase ( EC ). (
  • PKA is also commonly known as cAMP-dependent protein kinase, because it has traditionally been thought to be activated through release of the catalytic subunits when levels of the second messenger cAMP rise in response to a variety of signals. (
  • Hence, the synonym cAMP-dependent protein kinase is commonly used. (
  • The closest relatives of MAPKs are the cyclin-dependent kinases (CDKs). (
  • It is not to be confused with AMP-activated protein kinase or cyclin-dependent kinases . (
  • AMP-activated protein kinase (AMPK), an energy sensor, can regulate protein and lipid metabolism responding to alterations in energy supply. (
  • Migrating neurons also have intrinsic machineries to regulate cytoskeletal proteins and adhesion properties. (
  • Abl contains 407 amino acids (residues 237-643 of the p120-gag-abl polyprotein), which include the kinase catalytic domain, SH2 domain on the N-terminus and the I237M mutation. (
  • There are a number of conserved regions in the catalytic domain of protein kinases. (
  • Most protein kinases belong to a single superfamily containing a eukaryotic protein kinase (ePK) catalytic domain. (
  • The Plasmodium falciparum genome encodes a number of proteins putatively involved in calcium signaling, including calmodulin-related proteins, a calcium-transporting ATPase, and a family of CDPKs, which are composed of a protein kinase catalytic domain fused to a calcium-binding domain. (
  • A serine/threonine protein kinase ( EC ) is a kinase enzyme that phosphorylates the OH group of serine or threonine (which have similar sidechains). (
  • These were formerly included in EC number "", which was a general EC number for any enzyme that phosphorylates proteins while converting ATP to ADP (i.e. (
  • There are three tiers of protein kinases within each SAPK module, comprising of a MAPKKK which phosphorylates and activates a MAPKK, which in turn phosphorylates and activates the terminal SAPK. (
  • It phosphorylates tyrosine residues located in the C-terminal tails of Src-family kinases (SFKs). (
  • c-Src phosphorylates specific tyrosine residues in other tyrosine kinases. (
  • [4] In contrast to the classical MAP kinases, these atypical MAPKs require only a single residue in their activation loops to be phosphorylated. (
  • Four human protein kinases (underlined) representing the four major families in the CMGC group (CDKs, MAPKs, GSK3, and CDK-like) were included in the alignment to anchor the position of these families in the tree. (
  • In the case of classical MAP kinases, the activation loop contains a characteristic TxY (threonine-x-tyrosine) motif (TEY in mammalian ERK1 and ERK2 , TDY in ERK5 , TPY in JNKs , TGY in p38 kinases ) that needs to be phosphorylated on both the threonine and the tyrosine residues in order to lock the kinase domain in a catalytically competent conformation. (
  • A . Four residues from 25 human kinases and two ELKs (PknB and Aph) form the R-spine. (
  • B . Seven residues from 24 human kinases and one ELK (PknB) form the C-spine. (
  • The catalytic subunit contains the active site, a series of canonical residues found in protein kinases that bind and hydrolyse ATP and a domain to bind the regulatory subunit. (
  • Activity of MAP kinases is restricted by a number of protein phosphatases, which remove the phosphate groups that are added to specific serine or threonine residues of the kinase and are required to maintain the kinase in an active conformation. (
  • MGI protein superfamily detail pages represent the protein classification set for a homeomorphic superfamily from the Protein Information Resource SuperFamily ( PIRSF ) site. (
  • You can select a given mouse superfamily member and download (or forward to NCBI BLAST) FASTA formatted protein sequences of that mouse gene and its mouse, human and rat homologs, as defined in the corresponding HomoloGene Class. (
  • You can also "Select all" mouse superfamily members to obtain their protein sequences and the protein sequences for all mouse, human and rat homologs of the mouse superfamily members. (
  • For mouse superfamily members not included in any HomoloGene Class, only the mouse protein sequence is returned. (
  • 1.3 A Tour of the Human Protein Kinase Superfamily. (
  • We used a carefully constructed structural alignment of selected kinases as the basis for a study of the structural evolution of the protein kinase-like superfamily. (
  • Hence, the protein kinase-like superfamily has undergone substantial structural and sequence revision over long evolutionary timescales. (
  • While the PIPKs probably have an evolutionary relationship with the rest of the kinase superfamily, the relationship appears to be very distant (and perhaps indirect). (
  • The CDPK-SnRK superfamily consists of seven types of serine-threonine protein kinases: calcium-dependent protein kinase (CDPKs), CDPK-related kinases (CRKs), phospho enol pyruvate carboxylase kinases (PPCKs), PEP carboxylase kinase-related kinases (PEPRKs), calmodulin-dependent protein kinases (CaMKs), calcium and calmodulin-dependent protein kinases (CCaMKs), and SnRKs. (
  • In this report, we identify all of the kinases predicted to belong to the CDPK-SnRK superfamily based on the completed Arabidopsis genome sequence ( Arabidopsis Genome Initiative, 2000 ) and examine their evolutionary origins. (
  • We also present suggested nomenclature for all of the kinases in this superfamily. (
  • Compositions and methods are provided for the treatment and diagnosis of diseases associated with protein kinase C. Oligonucleotides are provided which are specifically hybridizable with a PKC gene or mRNA. (
  • Methods of treating conditions amenable to therapeutic intervention by modulating protein kinase C expression with an oligonucleotide specifically hybridizable with a PKC gene or mRNA are disclosed. (
  • Our findings establish PKM2 as a histone kinase, which directly regulates gene transcription and controls cell cycle progression and proliferation of tumor cells' Lu said. (
  • As the world's leading gene company, OriGene offers comprehensive product solutions for studying human protein kinases. (
  • In humans, this protein is encoded by the gene SRPK3. (
  • Tyrosine Protein Kinase CSK (C Src Kinase or Protein Tyrosine Kinase CYL or CSK or EC - Tyrosine-protein kinase CSK also known as C-terminal Src kinase is an enzyme that, in humans, is encoded by the CSK gene. (
  • It belongs to a family of Src family kinases and is similar to the v-Src (viral Src) gene of Rous sarcoma virus. (
  • Two transcript variants encoding the same protein have been found for this gene. (
  • 2. Phosphatases- an enzyme that removes a phosphate from a protein. (
  • 4.3 SRC and SRC Family Kinases. (
  • 5.3.2 RAF Family Kinases. (
  • Given the versatility inherent in this intrinsically disordered region, its multisite phosphorylations, and its divergence within the family, the unique domain likely functions as a central signaling hub overseeing much of the enzymatic activities and unique functions of Src family kinases. (
  • Similar to the SAPK/JNK pathway, p38 MAP kinase is activated by a variety of cellular stresses including osmotic shock, inflammatory cytokines, lipopolysaccharides (LPS), Ultraviolet light, and growth factors. (
  • The R 2 homodimer is formed by an N-terminal dimerization/docking (DD) domain that also mediates sub-cellular localization via A kinase anchoring proteins (AKAPs). (
  • Protein Kinase CK2 and Cellular Function in Normal and Disease States increases knowledge of the role of CK2 in the development of cellular dysfunction and emphasizes that this protein may serve as a target of drug development for improved cancer therapy. (
  • In eukaryotes, protein kinases are involved in regulating key aspects of cellular function, including cell division, metabolism, and responses to external signals. (
  • Changes were reported to be induced in the function of protein kinase C, cyclic AMP-dependent protein kinase, and calcium/calmodulin-dependent protein kinase. (
  • For two of these kinases (cyclic AMP- and calcium/calmodulin-dependent), the changes have been studied in isolated neuronal compartments (microtubules and presynaptic terminals). (
  • Protein kinase A, more precisely known as adenosine 3',5'-monophosphate (cyclic AMP)-dependent protein kinase was discovered by chemists Edmond H. Fischer and Edwin G. Krebs in 1968. (
  • Cloning and characterization of BCY1, a locus encoding a regulatory subunit of the cyclic AMP-dependent protein kinase in Saccharomyces cerevisiae. (
  • The chemical activity of a kinase involves removing a phosphate group from ATP and covalently attaching it to one of three amino acids that have a free hydroxyl group. (
  • Most protein kinases act on the amino acids serine and threonine, while tyrosine kinases act on tyrosine, and some protein kinases act on all three. (
  • We categorize protein kinases as either serine-threonine or tyrosine kinases based on the amino acids they modify. (
  • The intracellular or cytoplasmic domain is responsible for the (highly conserved) kinase activity, as well as several regulatory functions. (
  • A series of reactions, mediated by the intracellular serine/threonine kinase protein kinase A, which occurs as a result of a single trigger reaction or compound. (
  • LY 294002 was found to inhibit casein kinase-2 with similar potency to phosphoinositide (phosphatidylinositol) 3-kinase. (
  • Protein kinase CK2 (formerly casein kinase II or 2) is known to play a critical role in the control of cell growth and cell death and is thus intimately involved in the development of cancer. (
  • This group represents protein kinase C (KPC), including zeta/iota types from mammals, protein kinase C-like 3 from round worms [ PMID: 9422779 ] and atypical protein kinase C (aPKC) from fruit flies [ PMID: 10995441 ]. (
  • Structure, expression, and properties of an atypical protein kinase C (PKC3) from Caenorhabditis elegans. (
  • Drosophila atypical protein kinase C associates with Bazooka and controls polarity of epithelia and neuroblasts. (
  • Atypical protein kinase C is involved in the evolutionarily conserved par protein complex and plays a critical role in establishing epithelia-specific junctional structures. (
  • Atypical protein kinase C{iota} is required for bronchioalveolar stem cell expansion and lung tumorigenesis. (
  • 1.3.10 Atypical Protein Kinases. (
  • In addition, our analysis suggests that the actin-fragmin kinase, an atypical protein kinase, is more closely related to the phosphoinositide-3 kinase family than to the protein kinase family. (
  • Atypical protein kinase C (aPKC) is a key apical-basal polarity determinant and Par complex component. (
  • Working in cell lines and mouse models of glioblastoma multiforme, the most lethal form of brain tumor, senior author Zhimin Lu, Ph.D., associate professor of Neuro-Oncology at MD Anderson, and colleagues show that pyruvate kinase M2 (PKM2) fuels tumor growth by influencing a histone protein. (
  • The CDPK-related kinases (CRKs) and phospho enol pyruvate carboxylase kinase-related kinases (PEPRKs) are also unique to plants. (
  • In addition, the two major types of kinases that decode calcium signals in animals (calmodulin-dependent protein kinases [CaMKs] and protein kinase C) appear to be missing or under-represented in plants. (
  • Important subgroups are the kinases of the ERK subfamily, typically activated by mitogenic signals, and the stress-activated protein kinases JNK and p38. (
  • Curcumin has anti-breast cancer activity related to the activities of protein kinases on cell signal pathway. (
  • The catalytic subunits of many protein kinases are highly conserved, and several structures have been solved. (
  • CK2 is a ubiquitous and highly conserved protein serine / threonine kinase that has long been considered to play a role in cell growth and proliferation. (
  • To inhibit SFKs, CSK is recruited to the plasma membrane via binding to transmembrane proteins or adapter proteins located near the plasma membrane. (
  • During the course of evolution, protein kinases developed a universal regulatory mechanism associated with a large activation segment that can be dynamically folded and unfolded in the course of cell functioning. (
  • Protein kinase C zeta type is a calcium- and diacylglycerol-independent serine/threonine-protein kinase that functions in phosphatidylinositol 3-kinase (PI3K) pathway and mitogen-activated protein (MAP) kinase cascade, and is involved in NF-kappa-B activation, mitogenic signaling, cell proliferation, cell polarity, inflammatory response and maintenance of long-term potentiation (LTP) [ PMID: 11035106 ]. (
  • Protein kinase C zeta plays a central role in activation of the p42/44 mitogen-activated protein kinase by endotoxin in alveolar macrophages. (
  • Here we demonstrate that activation of these ubiquitously expressed MAP kinases is essential for growth. (
  • To specifically suppress MAP kinase activation in fibroblasts, we transiently expressed either the entire p44mapk antisense RNA or p44mapk kinase-deficient mutants (T192A or Y194F). (
  • As expected, and through independent mechanisms, both approaches strongly inhibited MAP kinase activation. (
  • Dr. Locniskar continued studying linoleic acid, an omega-6 polyunsaturated fatty acid, and the role it seems to play in protein kinase C activation and distribution, that is essential for normal cell communication. (
  • 4.5.1 Activation and Known Mutations and Fusions of the JAKFamily of Tyrosine Kinases. (
  • 5.5 Protein Kinase C. 5.5.1 PKC Activation. (
  • Protein kinase C activation and the development of diabetic complications. (
  • Recent studies have identified that the activation of protein kinase C (PKC) and increased diacylglycerol (DAG) levels initiated by hyperglycemia are associated with many vascular abnormalities in retinal, renal, and cardiovascular tissues. (
  • We have catalogued the protein kinase complement of the human genome (the "kinome") using public and proprietary genomic, complementary DNA, and expressed sequence tag (EST) sequences. (
  • With the advent of DNA cloning and sequencing in the mid-1970s, it rapidly became clear that a large family of eukaryotic protein kinases exists, and the burgeoning numbers of protein kinases led to the speculation that a vertebrate genome might encode as many as 1001 protein kinases ( 1 ). (
  • The near-completion of the human genome sequence now allows the identification of almost all human protein kinases. (
  • The figure depicts only the CMGC branch of a larger tree constructed (by J. Packer, Abbott Laboratories) from a Hidden Markov Model-derived alignment of all protein kinases in the P. falciparum genome. (
  • The presence of closely related kinases in regions of the genome known to have arisen by genome duplication indicates that these kinases probably arose by divergence from common ancestors. (
  • The completed sequence of the Arabidopsis genome provides the first opportunity to identify all of the protein kinases present in a model plant. (
  • We offer an extensive portfolio of highly active proteins and peptides, suitable for a wide range of applications to meet all of your research needs. (
  • Trust us to supply proteins and peptides with the high purity, activity, and specificity that your research demands. (
  • Lot-to-lot consistency and reliable performance make us the source for proteins and peptides you can count on. (
  • Bulk quantities of our proteins and peptides are available to meet your research or assay development needs. (
  • We offer Guanylate kinase Peptides and Guanylate kinase Proteins for use in common research applications: ELISA, Protein Array, SDS-Page, Western Blot. (
  • Our Guanylate kinase Peptides and Guanylate kinase Proteins can be used in a variety of model species: Human. (
  • Choose from our Guanylate kinase Peptides and Proteins. (
  • Transmembrane protein in contact with both cytoplasm and the extracellular environment. (
  • The Human siGENOME RTF Protein Kinase siRNA Library includes SMARTpool siRNA reagents directed against phylogenetically-related kinases. (
  • The Human siGENOME Protein Kinase siRNA Library includes siRNA reagents directed against phylogenetically-related kinases. (
  • Assay for Immunoprecipitated Phosphoinositide 3-Kinase (PI 3 Kinase) Activity (in vitro) Immunoprecipitation assay for Phosphoinositide 3-Kinase (PI 3 Kinase) Activity (in vitro) Protocol. (
  • Protein kinases thus represent a unique, highly dynamic, and precisely regulated set of switches that control most biological events in eukaryotic cells. (
  • Furthermore, IFN-γ-induced secretion was dependent on tyrosine protein kinase activity. (
  • Tyrosine Protein Kinase CSK (C Src Kinase or Protein Tyrosine Kinase CYL or CSK or EC pipeline Target constitutes close to 12 molecules. (
  • It also reviews key players involved in Tyrosine Protein Kinase CSK (C Src Kinase or Protein Tyrosine Kinase CYL or CSK or EC targeted therapeutics development with respective active and dormant or discontinued projects. (
  • MAP kinases are found in eukaryotes only, but they are fairly diverse and encountered in all animals, fungi and plants, and even in an array of unicellular eukaryotes. (
  • By this analysis, there were 53 distinct kinase functions in the early common ancestor of all these eukaryotes, and there has been much gain and loss since then. (
  • Conversely, the α-kinases appear to be an exception to the scenario of early divergence for the atypical kinases: they apparently arose relatively recently in eukaryotes. (
  • Our recombinant and natural proteins are tested in bioassays, as well as standard QC procedures, to ensure that you receive proteins that are highly biologically active. (
  • The possible role of protein kinase C (PKC) in regulating this critical transition was assessed in both normal oocytes isolated from small antral follicles (18-day-old B6SJLF1 mice), which have not yet developed the capacity to progress to metaphase II (MII), and also oocytes defective in their ability to exit MI despite development to the preovulatory stage (24-day-old CX8 recombinant inbred strains). (
  • These patterns, termed "spines", do not form sequential motifs coming from different parts of protein kinases sequence. (
  • The number of protein sequences returned does not always match the numbers of homologs shown, because the same protein sequence can be associated with multiple homologs. (
  • Note that the 'protein existence' evidence does not give information on the accuracy or correctness of the sequence(s) displayed. (
  • 10. An antisense oligonuclcotide 5 to 50 nucleotides in length comprising a nucleotide sequence which is complementary to the long mRNA transcript of human protein kinase C-α and which is not complementary to the short mRNA transcript of human protein kinase C-α. (
  • 13. A polynucleotide probe comprising a nuclcotide sequence complementary to the long mRNA transcript of human protein kinase C-α. (
  • 15. A method of inhibiting the expression of human protein kinase C-α in vitro comprising contacting human cells with a therapeutically effective amount of an antisense oligonucleotide 5 to 50 nucleotides in length, said antisense oligonucleotide comprising a nucleotide sequence complementary to a portion of the sequence set forth in SEQ ID NO: 105. (
  • Further details about individual kinases, including corrected sequence annotations, links to sequence alignments, and functional annotations, can be found at the PlantsP Web site ( ). (
  • Protein Kinase Protocols procedures and assays for kinase activity. (
  • Troubleshooting Tips for Immunoprecipitation / Kinase Assays Troubleshooting Tips for Immunoprecipitation / Kinase Assays. (
  • The Gs alpha subunit of the stimulated G protein complex exchanges GDP for GTP and is released from the complex. (
  • Four alleles of Cos1 appear to be dominant-negative mutations of a catalytic subunit of protein kinase A ( pka-C1 ) and the fifth allele, Cos1 A1 , is a gain-of-function allele of the PKA regulatory subunit pka-RII . (
  • In Protein Kinase Protocols, a panel of highly skilled laboratory investigators describe both basic and more sophisticated methods for the analysis of kinase-mediated signaling cascades, with emphasis on the identification of proteins according to their interactive relationships and the analysis of their functional properties. (
  • This profile is sensitive enough to detect short fragments of even very divergent kinases that have little similarity to any single known kinase. (
  • By whole-kinome comparisons, we can relate kinases across highly divergent organisms and track the birth, spread, expansion, and even death of kinases. (
  • The two most divergent families, α-kinases and phosphatidylinositol phosphate kinases (PIPKs), appear to have distinct evolutionary histories. (
  • Conversely, plants contain a number of kinase families that either are not found in animals or yeast or are highly divergent. (
  • Crizotinib is used for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) that is anaplastic-lymphoma kinase (ALK)-positive as detected by a FDA-approved test. (
  • 3.3 Anaplastic Lymphoma Kinase. (
  • Evolution of protein kinase signaling from yeast to man. (
  • These effects were proportional to the extent of MAP kinase inhibition and reversed by coexpression of the wild-type p44mapk. (
  • 1.5.2 Alternative Strategies for Kinase Inhibition. (
  • At least 125 of the 500+ human protein kinases are serine/threonine kinases (STK). (
  • New nucleic acid sequences are provided which encode 3' untranslated regions of human protein kinase C alpha polynucleotide probes for PKC alpha are also disclosed. (
  • Kinase dysfunction is also connected to a variety of human diseases including cancer, inflammatory conditions, autoimmune disorders, and cardiac diseases. (
  • A ready-to-use reverse transfection format RNAi screening library targeting human kinases. (
  • The OriGene True Clone collection has proven to be an excellent source of full-length human cDNAs for use in Regeneron's protein expression and target validation platforms. (
  • An arrayed siRNA collection targeting human kinases. (
  • Most kinases act on both serine and threonine, others act on tyrosine, and a number (dual-specificity kinases) act on all three. (
  • The protein product of proto-oncogene RAS can increase activity of p38, and thereby cause excessively high activity of transcription factor NF-κB. (
  • Because protein kinases have profound effects on a cell, their activity is highly regulated. (
  • Activity of these protein kinases can be regulated by specific events (e.g. (
  • Assay activity of Lck kinase expressed in a retroviral vector in rat fibroblasts. (
  • Protocol applicable only to kinases whose activity is not altered by cell lysis or immunoprecipitation procedures, and do not require soluble cofactors for activity. (
  • Protein kinases are key regulators of cell function and are known to direct the activity and function of many proteins. (
  • 2.3 Catalytic Activity of Protein Kinases. (
  • For this reason, the tyrosine kinase activity of the JAKs is carefully regulated at a number of different levels. (
  • Remarkably, even within the universal core some kinase structures display notable changes, while still retaining essential activity. (
  • It has been shown deregulation of kinase activity is a frequent cause of disease, particularly cancer. (
  • Kinases are a class of proteins that attach phosphate groups to other proteins. (
  • 1. Protein kinases- enzyme that adds phosphate groups from ATP to proteins. (
  • Aorta treated for 10 min with 4-phorbol 12-myristate 13-acetate (PMA), a protein kinase C activator, showed decreased relaxations to the endothelium-dependent vasodilator, acetylcholine, similar to normal aorta exposed to elevated glucose (22 and 44 mM) for 6 h. (