Adenylate Cyclase: An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC 4.6.1.1.Adenylate Cyclase Toxin: One of the virulence factors produced by virulent BORDETELLA organisms. It is a bifunctional protein with both ADENYLYL CYCLASES and hemolysin components.beta-Adrenergic Receptor Kinases: G-protein-coupled receptor kinases that mediate agonist-dependent PHOSPHORYLATION and desensitization of BETA-ADRENERGIC RECEPTORS.G-Protein-Coupled Receptor Kinase 2: A ubiquitously expressed G-protein-coupled receptor kinase subtype that has specificity for the agonist-occupied form of BETA-ADRENERGIC RECEPTORS. It may play an essential role in regulating myocardial contractile response.G-Protein-Coupled Receptor Kinases: A family of serine-threonine kinases that are specific for G-PROTEIN-COUPLED RECEPTORS. They are regulatory proteins that play a role in G-protein-coupled receptor densensitization.G-Protein-Coupled Receptor Kinase 5: A G-protein-coupled receptor kinase subtype that is primarily expressed in the MYOCARDIUM and may play a role in the regulation of cardiac functions.Cyclic AMP: 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.G-Protein-Coupled Receptor Kinase 3: A ubiquitously expressed G-protein-coupled receptor kinase subtype that has specificity for the agonist-occupied form of BETA-ADRENERGIC RECEPTORS and a variety of other G-PROTEIN-COUPLED RECEPTORS. Although it is highly homologous to G-PROTEIN-COUPLED RECEPTOR KINASE 2, it is not considered to play an essential role in regulating myocardial contractile response.GTP-Binding Proteins: Regulatory proteins that act as molecular switches. They control a wide range of biological processes including: receptor signaling, intracellular signal transduction pathways, and protein synthesis. Their activity is regulated by factors that control their ability to bind to and hydrolyze GTP to GDP. EC 3.6.1.-.Adenylate Kinase: An enzyme that catalyzes the phosphorylation of AMP to ADP in the presence of ATP or inorganic triphosphate. EC 2.7.4.3.Guanylate Cyclase: An enzyme that catalyzes the conversion of GTP to 3',5'-cyclic GMP and pyrophosphate. It also acts on ITP and dGTP. (From Enzyme Nomenclature, 1992) EC 4.6.1.2.Guanylyl Imidodiphosphate: A non-hydrolyzable analog of GTP, in which the oxygen atom bridging the beta to the gamma phosphate is replaced by a nitrogen atom. It binds tightly to G-protein in the presence of Mg2+. The nucleotide is a potent stimulator of ADENYLYL CYCLASES.Cyclic AMP-Dependent Protein Kinases: 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.Colforsin: Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.Protein Kinases: A family of enzymes that catalyze the conversion of ATP and a protein to ADP and a phosphoprotein.Guanosine Triphosphate: Guanosine 5'-(tetrahydrogen triphosphate). A guanine nucleotide containing three phosphate groups esterified to the sugar moiety.Enzyme Activation: 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.Pituitary Adenylate Cyclase-Activating Polypeptide: A multi-function neuropeptide that acts throughout the body by elevating intracellular cyclic AMP level via its interaction with PACAP RECEPTORS. Although first isolated from hypothalamic extracts and named for its action on the pituitary, it is widely distributed in the central and peripheral nervous systems. PACAP is important in the control of endocrine and homeostatic processes, such as secretion of pituitary and gut hormones and food intake.Virulence Factors, Bordetella: A set of BACTERIAL ADHESINS and TOXINS, BIOLOGICAL produced by BORDETELLA organisms that determine the pathogenesis of BORDETELLA INFECTIONS, such as WHOOPING COUGH. They include filamentous hemagglutinin; FIMBRIAE PROTEINS; pertactin; PERTUSSIS TOXIN; ADENYLATE CYCLASE TOXIN; dermonecrotic toxin; tracheal cytotoxin; Bordetella LIPOPOLYSACCHARIDES; and tracheal colonization factor.Isoproterenol: Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.Kinetics: The rate dynamics in chemical or physical systems.Protein-Serine-Threonine Kinases: A group of enzymes that catalyzes the phosphorylation of serine or threonine residues in proteins, with ATP or other nucleotides as phosphate donors.Fluorides: Inorganic salts of hydrofluoric acid, HF, in which the fluorine atom is in the -1 oxidation state. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed) Sodium and stannous salts are commonly used in dentifrices.Pertussis Toxin: One of the virulence factors produced by BORDETELLA PERTUSSIS. It is a multimeric protein composed of five subunits S1 - S5. S1 contains mono ADPribose transferase activity.Receptors, Adrenergic, beta: One of two major pharmacologically defined classes of adrenergic receptors. The beta adrenergic receptors play an important role in regulating CARDIAC MUSCLE contraction, SMOOTH MUSCLE relaxation, and GLYCOGENOLYSIS.Cell Membrane: The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.Signal Transduction: 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.Phosphatidylinositol 3-Kinases: 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.Cholera Toxin: An ENTEROTOXIN from VIBRIO CHOLERAE. It consists of two major protomers, the heavy (H) or A subunit and the B protomer which consists of 5 light (L) or B subunits. The catalytic A subunit is proteolytically cleaved into fragments A1 and A2. The A1 fragment is a MONO(ADP-RIBOSE) TRANSFERASE. The B protomer binds cholera toxin to intestinal epithelial cells, and facilitates the uptake of the A1 fragment. The A1 catalyzed transfer of ADP-RIBOSE to the alpha subunits of heterotrimeric G PROTEINS activates the production of CYCLIC AMP. Increased levels of cyclic AMP are thought to modulate release of fluid and electrolytes from intestinal crypt cells.Sodium Fluoride: A source of inorganic fluoride which is used topically to prevent dental caries.Phosphorylation: The introduction of a phosphoryl group into a compound through the formation of an ester bond between the compound and a phosphorus moiety.MAP Kinase Signaling System: 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.G-Protein-Coupled Receptor Kinase 1: A PROTEIN-SERINE-THREONINE KINASE that is found in PHOTORECEPTOR CELLS. It mediates light-dependent PHOSPHORYLATION of RHODOPSIN and plays an important role in PHOTOTRANSDUCTION.G-Protein-Coupled Receptor Kinase 4: A G-protein-coupled receptor kinase subtype that is primarily expressed in the TESTES and BRAIN. Variants of this subtype exist due to multiple alternative splicing of its mRNA.Molecular Sequence Data: 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.Cell Line: Established cell cultures that have the potential to propagate indefinitely.Protein Kinase C: 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.Amino Acid Sequence: 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.Alprostadil: A potent vasodilator agent that increases peripheral blood flow.Bordetella pertussis: A species of gram-negative, aerobic bacteria that is the causative agent of WHOOPING COUGH. Its cells are minute coccobacilli that are surrounded by a slime sheath.Guanosine 5'-O-(3-Thiotriphosphate): Guanosine 5'-(trihydrogen diphosphate), monoanhydride with phosphorothioic acid. A stable GTP analog which enjoys a variety of physiological actions such as stimulation of guanine nucleotide-binding proteins, phosphoinositide hydrolysis, cyclic AMP accumulation, and activation of specific proto-oncogenes.Protein Kinase Inhibitors: Agents that inhibit PROTEIN KINASES.Heterotrimeric GTP-Binding Proteins: GTP-BINDING PROTEINS that contain three non-identical subunits. They are found associated with members of the seven transmembrane domain superfamily of G-PROTEIN-COUPLED RECEPTORS. Upon activation the GTP-BINDING PROTEIN ALPHA SUBUNIT of the complex dissociates leaving a dimer of a GTP-BINDING PROTEIN BETA SUBUNIT bound to a GTP-BINDING PROTEIN GAMMA SUBUNIT.Calcium-Calmodulin-Dependent Protein Kinases: 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)Thionucleotides: Nucleotides in which the base moiety is substituted with one or more sulfur atoms.Adenosine Diphosphate Ribose: An ester formed between the aldehydic carbon of RIBOSE and the terminal phosphate of ADENOSINE DIPHOSPHATE. It is produced by the hydrolysis of nicotinamide-adenine dinucleotide (NAD) by a variety of enzymes, some of which transfer an ADP-ribosyl group to target proteins.Receptors, Cell Surface: Cell surface proteins that bind signalling molecules external to the cell with high affinity and convert this extracellular event into one or more intracellular signals that alter the behavior of the target cell (From Alberts, Molecular Biology of the Cell, 2nd ed, pp693-5). Cell surface receptors, unlike enzymes, do not chemically alter their ligands.Guanine NucleotidesProtein-Tyrosine Kinases: Protein kinases that catalyze the PHOSPHORYLATION of TYROSINE residues in proteins with ATP or other nucleotides as phosphate donors.src-Family Kinases: 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.1-Methyl-3-isobutylxanthine: A potent cyclic nucleotide phosphodiesterase inhibitor; due to this action, the compound increases cyclic AMP and cyclic GMP in tissue and thereby activates CYCLIC NUCLEOTIDE-REGULATED PROTEIN KINASESReceptor Protein-Tyrosine Kinases: A class of cellular receptors that have an intrinsic PROTEIN-TYROSINE KINASE activity.Cells, Cultured: 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.Mutation: 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.Calcium: 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.Prostaglandins E: (11 alpha,13E,15S)-11,15-Dihydroxy-9-oxoprost-13-en-1-oic acid (PGE(1)); (5Z,11 alpha,13E,15S)-11,15-dihydroxy-9-oxoprosta-5,13-dien-1-oic acid (PGE(2)); and (5Z,11 alpha,13E,15S,17Z)-11,15-dihydroxy-9-oxoprosta-5,13,17-trien-1-oic acid (PGE(3)). Three of the six naturally occurring prostaglandins. They are considered primary in that no one is derived from another in living organisms. Originally isolated from sheep seminal fluid and vesicles, they are found in many organs and tissues and play a major role in mediating various physiological activities.Receptors, Adrenergic: Cell-surface proteins that bind epinephrine and/or norepinephrine with high affinity and trigger intracellular changes. The two major classes of adrenergic receptors, alpha and beta, were originally discriminated based on their cellular actions but now are distinguished by their relative affinity for characteristic synthetic ligands. Adrenergic receptors may also be classified according to the subtypes of G-proteins with which they bind; this scheme does not respect the alpha-beta distinction.Arrestins: Regulatory proteins that down-regulate phosphorylated G-protein membrane receptors, including rod and cone photoreceptors and adrenergic receptors.Protein Binding: 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.Dideoxyadenosine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is an inhibitor of HIV replication, acting as a chain-terminator of viral DNA by binding to reverse transcriptase. Its principal side effect is nephrotoxicity. In vivo, dideoxyadenosine is rapidly metabolized to DIDANOSINE (ddI) by enzymatic deamination; ddI is then converted to dideoxyinosine monophosphate and ultimately to dideoxyadenosine triphosphate, the putative active metabolite.Cattle: 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.Transfection: 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.GTP-Binding Protein alpha Subunits, Gi-Go: A family of heterotrimeric GTP-binding protein alpha subunits that were originally identified by their ability to inhibit ADENYLYL CYCLASES. Members of this family can couple to beta and gamma G-protein subunits that activate POTASSIUM CHANNELS. The Gi-Go part of the name is also spelled Gi/Go.Epinephrine: The active sympathomimetic hormone from the ADRENAL MEDULLA. It stimulates both the alpha- and beta- adrenergic systems, causes systemic VASOCONSTRICTION and gastrointestinal relaxation, stimulates the HEART, and dilates BRONCHI and cerebral vessels. It is used in ASTHMA and CARDIAC FAILURE and to delay absorption of local ANESTHETICS.Mitogen-Activated Protein Kinase 1: 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.GTP-Binding Protein beta Subunits: Heterotrimeric GTP-binding protein subunits that tightly associate with GTP-BINDING PROTEIN GAMMA SUBUNITS. A dimer of beta and gamma subunits is formed when the GTP-BINDING PROTEIN ALPHA SUBUNIT dissociates from the GTP-binding protein heterotrimeric complex. The beta-gamma dimer can play an important role in signal transduction by interacting with a variety of second messengers.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.p38 Mitogen-Activated Protein Kinases: 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.Glucagon: A 29-amino acid pancreatic peptide derived from proglucagon which is also the precursor of intestinal GLUCAGON-LIKE PEPTIDES. Glucagon is secreted by PANCREATIC ALPHA CELLS and plays an important role in regulation of BLOOD GLUCOSE concentration, ketone metabolism, and several other biochemical and physiological processes. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1511)Binding Sites: The parts of a macromolecule that directly participate in its specific combination with another molecule.GTP-Binding Protein alpha Subunits: The GTPase-containing subunits of heterotrimeric GTP-binding proteins. When dissociated from the heterotrimeric complex these subunits interact with a variety of second messenger systems. Hydrolysis of GTP by the inherent GTPase activity of the subunit causes it to revert to its inactive (heterotrimeric) form. The GTP-Binding protein alpha subunits are grouped into families according to the type of action they have on second messenger systems.Recombinant Proteins: Proteins prepared by recombinant DNA technology.Vasoactive Intestinal Peptide: A highly basic, 28 amino acid neuropeptide released from intestinal mucosa. It has a wide range of biological actions affecting the cardiovascular, gastrointestinal, and respiratory systems and is neuroprotective. It binds special receptors (RECEPTORS, VASOACTIVE INTESTINAL PEPTIDE).GTP-Binding Protein alpha Subunits, Gs: A family of heterotrimeric GTP-binding protein alpha subunits that activate ADENYLYL CYCLASES.Base Sequence: The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.Adenosine Triphosphate: 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.Receptor, Insulin: A cell surface receptor for INSULIN. It comprises a tetramer of two alpha and two beta subunits which are derived from cleavage of a single precursor protein. The receptor contains an intrinsic TYROSINE KINASE domain that is located within the beta subunit. Activation of the receptor by INSULIN results in numerous metabolic changes including increased uptake of GLUCOSE into the liver, muscle, and ADIPOSE TISSUE.RGS Proteins: A large family of evolutionarily conserved proteins that function as negative regulators of HETEROTRIMERIC GTP-BINDING PROTEINS. RGS PROTEINS act by increasing the GTPase activity of the G alpha subunit of a heterotrimeric GTP-binding protein, causing it to revert to its inactive (GDP-bound) form.Phenylisopropyladenosine: N-Isopropyl-N-phenyl-adenosine. Antilipemic agent. Synonym: TH 162.Mitogen-Activated Protein Kinase 3: 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.Diterpenes: Twenty-carbon compounds derived from MEVALONIC ACID or deoxyxylulose phosphate.Calmodulin: 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.Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide, Type IIsoenzymes: Structurally related forms of an enzyme. Each isoenzyme has the same mechanism and classification, but differs in its chemical, physical, or immunological characteristics.Cricetinae: A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.GTP-Binding Protein gamma Subunits: Heterotrimeric GTP-binding protein subunits that tightly associate with GTP-BINDING PROTEIN BETA SUBUNITS. A dimer of beta and gamma subunits is formed when the GTP-BINDING PROTEIN ALPHA SUBUNIT dissociates from the GTP-binding protein heterotrimeric complex. The beta-gamma dimer can play an important role in signal transduction by interacting with a variety of second messengers.Turkeys: Large woodland game BIRDS in the subfamily Meleagridinae, family Phasianidae, order GALLIFORMES. Formerly they were considered a distinct family, Melegrididae.3',5'-Cyclic-AMP Phosphodiesterases: Enzymes that catalyze the hydrolysis of CYCLIC AMP to form adenosine 5'-phosphate. The enzymes are widely distributed in animal tissue and control the level of intracellular cyclic AMP. Many specific enzymes classified under this heading demonstrate additional spcificity for 3',5'-cyclic IMP and CYCLIC GMP.Iodocyanopindolol: A highly selective and specific beta antagonist that is used to characterize beta-adrenoceptors.Rats, Inbred Strains: Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding.Mitogen-Activated Protein Kinase Kinases: 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.Receptors, G-Protein-Coupled: The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.Guanosine Diphosphate: A guanine nucleotide containing two phosphate groups esterified to the sugar moiety.8-Bromo Cyclic Adenosine Monophosphate: 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.JNK Mitogen-Activated Protein Kinases: 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.Dihydroalprenolol: Hydrogenated alprenolol derivative where the extra hydrogens are often tritiated. This radiolabeled form of ALPRENOLOL, a beta-adrenergic blocker, is used to label the beta-adrenergic receptor for isolation and study.Cloning, Molecular: 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.Cyclic GMP: 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)p21-Activated Kinases: 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.Second Messenger Systems: Systems in which an intracellular signal is generated in response to an intercellular primary messenger such as a hormone or neurotransmitter. They are intermediate signals in cellular processes such as metabolism, secretion, contraction, phototransduction, and cell growth. Examples of second messenger systems are the adenyl cyclase-cyclic AMP system, the phosphatidylinositol diphosphate-inositol triphosphate system, and the cyclic GMP system.Type C Phospholipases: 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 3.1.4.3), it is commonly used in the literature to refer to broad variety of enzymes that specifically catalyze the hydrolysis of PHOSPHATIDYLINOSITOLS.Receptors, Muscarinic: One of the two major classes of cholinergic receptors. Muscarinic receptors were originally defined by their preference for MUSCARINE over NICOTINE. There are several subtypes (usually M1, M2, M3....) that are characterized by their cellular actions, pharmacology, and molecular biology.Time Factors: Elements of limited time intervals, contributing to particular results or situations.Recombinant Fusion 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.Enzyme Inhibitors: Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.Creatine Kinase: 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.Adrenergic beta-Agonists: Drugs that selectively bind to and activate beta-adrenergic receptors.Magnesium: A metallic element that has the atomic symbol Mg, atomic number 12, and atomic weight 24.31. It is important for the activity of many enzymes, especially those involved in OXIDATIVE PHOSPHORYLATION.Neuropeptides: Peptides released by NEURONS as intercellular messengers. Many neuropeptides are also hormones released by non-neuronal cells.Tetradecanoylphorbol Acetate: A phorbol ester found in CROTON OIL with very effective tumor promoting activity. It stimulates the synthesis of both DNA and RNA.Blotting, Western: 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.RNA, Messenger: 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.Receptors, Adrenergic, beta-2: A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The adrenergic beta-2 receptors are more sensitive to EPINEPHRINE than to NOREPINEPHRINE and have a high affinity for the agonist TERBUTALINE. They are widespread, with clinically important roles in SKELETAL MUSCLE; LIVER; and vascular, bronchial, gastrointestinal, and genitourinary SMOOTH MUSCLE.Tyrosine: A non-essential amino acid. In animals it is synthesized from PHENYLALANINE. It is also the precursor of EPINEPHRINE; THYROID HORMONES; and melanin.Molecular Weight: The sum of the weight of all the atoms in a molecule.Sequence Homology, Amino Acid: The degree of similarity between sequences of amino acids. This information is useful for the analyzing genetic relatedness of proteins and species.GTP Phosphohydrolases: Enzymes that hydrolyze GTP to GDP. EC 3.6.1.-.Pindolol: A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638)Receptors, Pituitary Hormone: Cell surface proteins that bind pituitary hormones with high affinity and trigger intracellular changes influencing the behavior of cells. Since many pituitary hormones are also released by neurons as neurotransmitters, these receptors are also found in the nervous system.Benzyl Alcohol: A colorless liquid with a sharp burning taste and slight odor. It is used as a local anesthetic and to reduce pain associated with LIDOCAINE injection. Also, it is used in the manufacture of other benzyl compounds, as a pharmaceutic aid, and in perfumery and flavoring.MAP Kinase Kinase Kinases: 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).CHO Cells: CELL LINE derived from the ovary of the Chinese hamster, Cricetulus griseus (CRICETULUS). The species is a favorite for cytogenetic studies because of its small chromosome number. The cell line has provided model systems for the study of genetic alterations in cultured mammalian cells.Mitogen-Activated Protein Kinases: 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).Binding, Competitive: The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.Theophylline: A methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant activities. Theophylline inhibits the 3',5'-CYCLIC NUCLEOTIDE PHOSPHODIESTERASE that degrades CYCLIC AMP thus potentiates the actions of agents that act through ADENYLYL CYCLASES and cyclic AMP.GTP-Binding Protein alpha Subunits, Gq-G11: A family of heterotrimeric GTP-binding protein alpha subunits that activate TYPE C PHOSPHOLIPASES dependent signaling pathways. The Gq-G11 part of the name is also spelled Gq/G11.Adenosine: A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.Substrate Specificity: A characteristic feature of enzyme activity in relation to the kind of substrate on which the enzyme or catalytic molecule reacts.Extracellular Signal-Regulated MAP Kinases: 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.Benzyl Alcohols: Alcohols derived from the aryl radical (C6H5CH2-) and defined by C6H5CHOH. The concept includes derivatives with any substituents on the benzene ring.PhosphoproteinsStructure-Activity Relationship: The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.GTP-Binding Protein Regulators: Proteins that regulate the signaling activity of GTP-BINDING PROTEINS. They are divided into three categories depending upon whether they stimulate GTPase activity (GTPASE-ACTIVATING PROTEINS), inhibit release of GDP; (GUANINE NUCLEOTIDE DISSOCIATION INHIBITORS); or exchange GTP for GDP; (GUANINE NUCLEOTIDE EXCHANGE FACTORS).Liver: A large lobed glandular organ in the abdomen of vertebrates that is responsible for detoxification, metabolism, synthesis and storage of various substances.Rabbits: 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.CDC2 Protein Kinase: 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.Protein Structure, Tertiary: 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.Rats, Sprague-Dawley: 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.Cyclin-Dependent Kinases: 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.Tumor Cells, Cultured: 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.Macromolecular Substances: Compounds and molecular complexes that consist of very large numbers of atoms and are generally over 500 kDa in size. In biological systems macromolecular substances usually can be visualized using ELECTRON MICROSCOPY and are distinguished from ORGANELLES by the lack of a membrane structure.Bucladesine: A cyclic nucleotide derivative that mimics the action of endogenous CYCLIC AMP and is capable of permeating the cell membrane. It has vasodilator properties and is used as a cardiac stimulant. (From Merck Index, 11th ed)Models, Biological: 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.Immunoblotting: 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.Receptors, Purinergic: Cell surface proteins that bind PURINES with high affinity and trigger intracellular changes which influence the behavior of cells. The best characterized classes of purinergic receptors in mammals are the P1 receptors, which prefer ADENOSINE, and the P2 receptors, which prefer ATP or ADP.Membrane Proteins: 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.Myocardium: 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.Insulin: 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).Transducin: A heterotrimeric GTP-binding protein that mediates the light activation signal from photolyzed rhodopsin to cyclic GMP phosphodiesterase and is pivotal in the visual excitation process. Activation of rhodopsin on the outer membrane of rod and cone cells causes GTP to bind to transducin followed by dissociation of the alpha subunit-GTP complex from the beta/gamma subunits of transducin. The alpha subunit-GTP complex activates the cyclic GMP phosphodiesterase which catalyzes the hydrolysis of cyclic GMP to 5'-GMP. This leads to closure of the sodium and calcium channels and therefore hyperpolarization of the rod cells. EC 3.6.1.-.Receptors, Vasoactive Intestinal Peptide: Cell surface proteins that bind VASOACTIVE INTESTINAL PEPTIDE; (VIP); with high affinity and trigger intracellular changes which influence the behavior of cells.eIF-2 Kinase: 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.Pyruvate Kinase: 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 2.7.1.40.Proto-Oncogene Proteins: 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.Mutagenesis, Site-Directed: Genetically engineered MUTAGENESIS at a specific site in the DNA molecule that introduces a base substitution, or an insertion or deletion.Casein Kinase II: 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.Casein Kinases: 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.Phosphoric Diester Hydrolases: A class of enzymes that catalyze the hydrolysis of one of the two ester bonds in a phosphodiester compound. EC 3.1.4.Carbachol: A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.Alprenolol: One of the ADRENERGIC BETA-ANTAGONISTS used as an antihypertensive, anti-anginal, and anti-arrhythmic agent.Electrophoresis, Polyacrylamide Gel: Electrophoresis in which a polyacrylamide gel is used as the diffusion medium.Peptides: 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.Ribosomal Protein S6 Kinases: 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.Blood Platelets: Non-nucleated disk-shaped cells formed in the megakaryocyte and found in the blood of all mammals. They are mainly involved in blood coagulation.Cytosol: Intracellular fluid from the cytoplasm after removal of ORGANELLES and other insoluble cytoplasmic components.Rhodopsin: A purplish-red, light-sensitive pigment found in RETINAL ROD CELLS of most vertebrates. It is a complex consisting of a molecule of ROD OPSIN and a molecule of 11-cis retinal (RETINALDEHYDE). Rhodopsin exhibits peak absorption wavelength at about 500 nm.Manganese: A trace element with atomic symbol Mn, atomic number 25, and atomic weight 54.94. It is concentrated in cell mitochondria, mostly in the pituitary gland, liver, pancreas, kidney, and bone, influences the synthesis of mucopolysaccharides, stimulates hepatic synthesis of cholesterol and fatty acids, and is a cofactor in many enzymes, including arginase and alkaline phosphatase in the liver. (From AMA Drug Evaluations Annual 1992, p2035)Stimulation, Chemical: The increase in a measurable parameter of a PHYSIOLOGICAL PROCESS, including cellular, microbial, and plant; immunological, cardiovascular, respiratory, reproductive, urinary, digestive, neural, musculoskeletal, ocular, and skin physiological processes; or METABOLIC PROCESS, including enzymatic and other pharmacological processes, by a drug or other chemical.Adenosine Monophosphate: Adenine nucleotide containing one phosphate group esterified to the sugar moiety in the 2'-, 3'-, or 5'-position.Aluminum Compounds: Inorganic compounds that contain aluminum as an integral part of the molecule.Receptor, Epidermal Growth Factor: A cell surface receptor involved in regulation of cell growth and differentiation. It is specific for EPIDERMAL GROWTH FACTOR and EGF-related peptides including TRANSFORMING GROWTH FACTOR ALPHA; AMPHIREGULIN; and HEPARIN-BINDING EGF-LIKE GROWTH FACTOR. The binding of ligand to the receptor causes activation of its intrinsic tyrosine kinase activity and rapid internalization of the receptor-ligand complex into the cell.Phosphotransferases: A rather large group of enzymes comprising not only those transferring phosphate but also diphosphate, nucleotidyl residues, and others. These have also been subdivided according to the acceptor group. (From Enzyme Nomenclature, 1992) EC 2.7.MAP Kinase Kinase 1: An abundant 43-kDa mitogen-activated protein kinase kinase subtype with specificity for MITOGEN-ACTIVATED PROTEIN KINASE 1 and MITOGEN-ACTIVATED PROTEIN KINASE 3.Serine: 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.Gene Expression: The phenotypic manifestation of a gene or genes by the processes of GENETIC TRANSCRIPTION and GENETIC TRANSLATION.Arabidopsis Proteins: Proteins that originate from plants species belonging to the genus ARABIDOPSIS. The most intensely studied species of Arabidopsis, Arabidopsis thaliana, is commonly used in laboratory experiments.Propranolol: A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.Gene Expression Regulation: 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.Thymidine Kinase: 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 2.7.1.21.Brassinosteroids: Plant steroids ubiquitously distributed throughout the plant kingdom. They play essential roles in modulating growth and differentiation of cells at nanomolar to micromolar concentrations.MAP Kinase Kinase 4: 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.Brain: The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.Escherichia coli: A species of gram-negative, facultatively anaerobic, rod-shaped bacteria (GRAM-NEGATIVE FACULTATIVELY ANAEROBIC RODS) commonly found in the lower part of the intestine of warm-blooded animals. It is usually nonpathogenic, but some strains are known to produce DIARRHEA and pyogenic infections. Pathogenic strains (virotypes) are classified by their specific pathogenic mechanisms such as toxins (ENTEROTOXIGENIC ESCHERICHIA COLI), etc.Phosphotransferases (Alcohol Group Acceptor): A group of enzymes that transfers a phosphate group onto an alcohol group acceptor. EC 2.7.1.DNA Primers: 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.Cell Division: The fission of a CELL. It includes CYTOKINESIS, when the CYTOPLASM of a cell is divided, and CELL NUCLEUS DIVISION.Sequence Alignment: The arrangement of two or more amino acid or base sequences from an organism or organisms in such a way as to align areas of the sequences sharing common properties. The degree of relatedness or homology between the sequences is predicted computationally or statistically based on weights assigned to the elements aligned between the sequences. This in turn can serve as a potential indicator of the genetic relatedness between the organisms.Inositol Phosphates: Phosphoric acid esters of inositol. They include mono- and polyphosphoric acid esters, with the exception of inositol hexaphosphate which is PHYTIC ACID.Down-Regulation: 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.1-Phosphatidylinositol 4-Kinase: 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.4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone: Inhibitor of phosphodiesterases.rho-Associated Kinases: 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.Phosphodiesterase Inhibitors: Compounds which inhibit or antagonize the biosynthesis or actions of phosphodiesterases.DNA, Complementary: 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.Precipitin Tests: 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.Glucose: A primary source of energy for living organisms. It is naturally occurring and is found in fruits and other parts of plants in its free state. It is used therapeutically in fluid and nutrient replacement.Steroids, Heterocyclic: Steroidal compounds in which one or more carbon atoms in the steroid ring system have been substituted with non-carbon atoms.Fluphenazine: A phenothiazine used in the treatment of PSYCHOSES. Its properties and uses are generally similar to those of CHLORPROMAZINE.Arabidopsis: A plant genus of the family BRASSICACEAE that contains ARABIDOPSIS PROTEINS and MADS DOMAIN PROTEINS. The species A. thaliana is used for experiments in classical plant genetics as well as molecular genetic studies in plant physiology, biochemistry, and development.Glycogen Synthase Kinase 3: 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.Protein Transport: 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.Cyclic GMP-Dependent Protein Kinases: A group of cyclic GMP-dependent enzymes that catalyze the phosphorylation of SERINE or THREONINE residues of proteins.

*Alamethicin

... beta-adrenergic receptor-coupled adenylate cyclase, and cAMP-dependent protein kinase activities of cardiac sarcolemmal ... domain before being attached by a thioester bond to an Acyl Carrier Protein-like Peptidyl carrier protein. The growing chain is ... Explore structures of Alamethicin at the protein data bank Alamethicin in Norine From "A voltage-gated ion channel model ... Amino acids are initially adenylated by an "adenylylation" (A) ...

*Histamine H2 receptor

H2 receptors are positively coupled to adenylate cyclase via Gs. It is a potent stimulant of cAMP production, which leads to ... involvement of a select array of G protein-coupled receptor kinases". Molecular Pharmacology. 60 (5): 1049-56. PMID 11641433. ... The histamine receptor H2 belongs to the rhodopsin-like family of G protein-coupled receptors. It is an integral membrane ... "Inhibition of H2 histamine receptor-mediated cation channel opening by protein kinase C in human promyelocytic cells". Journal ...

*Bradykinin receptor

... coupled to Gq and Gi. Gq stimulates phospholipase C to increase intracellular free calcium and Gi inhibits adenylate cyclase. ... Furthermore, the receptor stimulates the mitogen-activated protein kinase pathways. It is ubiquitously and constitutively ... There are two Bradykinin receptors: the B1 receptor and the B2 receptor. Bradykinin receptor B1 (B1) is a G-protein coupled ... The bradykinin receptor family is a group of G-protein coupled receptors whose principal ligand is the protein bradykinin. ...

*Glycogen phosphorylase

Glucagon activates adenylate cyclase through a seven transmembrane receptor coupled to Gs which, in turn, activates adenylate ... cAMP binds to and releases an active form of protein kinase A (PKA). Next, PKA phosphorylates phosphorylase kinase, which, in ... In the liver, glucagon activates another G-protein-linked receptor that triggers a different cascade, resulting in the ... This lack of easy access of the catalytic site to the surface is significant in that it makes the protein activity highly ...

*Bradykinin receptor B2

... is a G-protein coupled receptor for bradykinin, encoded by the BDKRB2 gene in humans. The B2 receptor is ... Gq stimulates phospholipase C to increase intracellular free calcium and Gi inhibits adenylate cyclase. Furthermore, the ... "Protein kinases A and C rapidly modulate expression of human lung fibroblast B2 bradykinin receptor affinity forms". Eur. J. ... 1999). "Endothelial nitric oxide synthase interactions with G-protein-coupled receptors". Biochem. J. 343 (2): 335-40. doi: ...

*Cannabinoid receptor type 1

Alternatively, in some rare cases CB1 receptor activation may be coupled to Gs proteins, which stimulate adenylate cyclase. ... adenylate cyclase, and increases mitogen-activated protein kinase (MAP kinase) concentration. ... The cannabinoid type 1 receptor, often abbreviated as CB1, is a G protein-coupled cannabinoid receptor located primarily in the ... Research suggests that the majority of CB1 receptors are coupled through Gi/o proteins. Upon activation, CB1 receptor exhibits ...

*Adenosine triphosphate

ATP is also a substrate of adenylate cyclase, most commonly in G protein-coupled receptor signal transduction pathways and is ... Phosphorylation of a protein by a kinase can activate a cascade such as the mitogen-activated protein kinase cascade. ... Kinases are the most common ATP-binding proteins. They share a small number of common folds. ... Scheeff, E.; Bourne, P. (2005). "Structural evolution of the protein kinase-like superfamily". PLoS Comput. Biol. 1 (5): e49. ...

*Lipolysis

G protein-coupled receptors) on the adipocyte cell membrane, which activate adenylate cyclase. This results in increased ... Insulin receptors activate insulin-like receptor substrates. These substrates activate phosphoinositide 3-kinases (PI-3K) which ... Lipolysis can be regulated through cAMP's binding and activation of protein kinase A (PKA). PKA can phosphorylate lipases, ... Perilipin 1A is a key protein regulator of lipolysis in adipose tissue. This lipid droplet-associated protein, when deactivated ...

*Skin whitening

... the hormone activates adenylate cyclase (AC) to produce cAMP as an intracellular second message via a G-protein-coupled ... receptor (GPCR)-type activation. cAMP activates protein kinase A (PKA), which then activates the gene expression of MITF via ... "Protease-activated receptor (PAR)-2 is a member of a novel G-protein-coupled seven-transmembrane receptor family. In epidermis ... The melanocortin 1 receptor (MC1R) is a transmembrane and G-protein coupled receptor expressed in melanocytes. MC1R is an ...

*Angiotensin II receptor type 1

Activated receptor also inhibits adenylate cyclase and activates various tyrosine kinases. The AT1 receptor may play role in ... Angiotensin II receptor type 1 has been shown to interact with Zinc finger and BTB domain-containing protein 16. The protein's ... The angiotensin receptor is activated by the vasoconstricting peptide angiotensin II. The activated receptor in turn couples to ... Angiotensin II receptor type 1 or AT1 receptor is the best characterized angiotensin receptor. It has vasopressor effects and ...

*Adrenergic receptor

All three are linked to Gs proteins (although β2 also couples to Gi), which in turn are linked to adenylate cyclase. Agonist ... Beta adrenergic receptor kinase Beta adrenergic receptor kinase-2 Cannon WB, Rosenbluth A (31 May 1933). "Studies On Conditions ... a Gq coupled receptor) and α2 (a Gi coupled receptor). Phenylephrine is a selective agonist of the α receptor. β receptors have ... α1-adrenergic receptors are members of the Gq protein-coupled receptor superfamily. Upon activation, a heterotrimeric G protein ...

*Angiotensin II receptor

Activated receptor also inhibits adenylate cyclase and activates various tyrosine kinases. Effects mediated by the AT1 receptor ... The angiotensin II receptors, (AGTR1) and (AGTR2), are a class of G protein-coupled receptors with angiotensin II as their ... The angiotensin receptor is activated by the vasoconstricting peptide angiotensin II. The activated receptor in turn couples to ... The AT1 receptor is the best elucidated angiotensin receptor. The AT1 subtype is found in the heart, blood vessels, kidney, ...

*Cyclic adenosine monophosphate

... protein-coupled receptors. Adenylate cyclase is inhibited by agonists of adenylate cyclase inhibitory G (Gi)-protein-coupled ... Not all protein kinases respond to cAMP. Several classes of protein kinases, including protein kinase C, are not cAMP-dependent ... Adenylate cyclase is activated by a range of signaling molecules through the activation of adenylate cyclase stimulatory G (Gs ... receptors. Liver adenylate cyclase responds more strongly to glucagon, and muscle adenylate cyclase responds more strongly to ...

*Muscarinic acetylcholine receptor M5

"Phosphorylation of human m1 muscarinic acetylcholine receptors by G protein-coupled receptor kinase 2 and protein kinase C". J ... of the endogenous ligand acetylcholine to the M5 receptor triggers a number of cellular responses such as adenylate cyclase ... is a member of the G protein-coupled receptor superfamily of integral membrane proteins. It is coupled to Gq protein. Binding ... "Signaling through transforming G protein-coupled receptors in NIH 3T3 cells involves c-Raf activation. Evidence for a protein ...

*Glucagon (medication)

Adenylate cyclase manufactures cyclic adenosine monophosphate (cyclic AMP or cAMP), which activates protein kinase A (cAMP- ... a G protein-coupled receptor, located in the plasma membrane. The conformation change in the receptor activates G proteins, a ... dependent protein kinase). This enzyme, in turn, activates phosphorylase kinase, which then phosphorylates glycogen ... When the G protein interacts with the receptor, it undergoes a conformational change that results in the replacement of the GDP ...

*Glucagon

Adenylate cyclase manufactures cyclic adenosine monophosphate (cyclic AMP or cAMP), which activates protein kinase A (cAMP- ... a G protein-coupled receptor, located in the plasma membrane. The conformation change in the receptor activates G proteins, a ... Layden BT, Durai V, Lowe WL (2010). "G-Protein-Coupled Receptors, Pancreatic Islets, and Diabetes". Nature Education. 3 (9): 13 ... dependent protein kinase). This enzyme, in turn, activates phosphorylase kinase, which then phosphorylates glycogen ...

*Glycogenesis

Epinephrine binds to a receptor protein that activates adenylate cyclase. The latter enzyme causes the formation of cyclic AMP ... G-Protein coupled receptor). When insulin binds to its receptor (insulin receptor), it results in the activation ( ... This latter enzyme is itself activated by protein kinase A and deactivated by phosphoprotein phosphatase-1. Protein kinase A ... This inhibition is achieved by a similar mechanism, as protein kinase A acts to phosphorylate the enzyme, which lowers activity ...

*G protein-coupled receptor

... via adenylate cyclase and cyclic AMP (cAMP). In a feedback mechanism, these activated kinases phosphorylate the receptor. The ... The G protein-coupled receptor kinases (GRKs) are protein kinases that phosphorylate only active GPCRs. G-protein-coupled ... receptor domain by protein kinases. Cyclic AMP-dependent protein kinases (protein kinase A) are activated by the signal chain ... 7TM receptors, heptahelical receptors, serpentine receptor, and G protein-linked receptors (GPLR), constitute a large protein ...

*Discovery and development of beta2 agonists

... and protein kinase A (PKA). The coupling of the β2-receptor to adenylate cyclase is affected through a trimeric Gs protein, as ... β-receptors are membrane-bound receptors coupled to G-proteins. Three types of β-receptors have been identified by molecular ... β3 receptors, which are presumed to be involved in fatty acid metabolism, are located in the adipocytes. G-protein coupled ... which stimulates adenylate cyclase) and βγ-subunits (which transduce other signals). Adenylate cyclase catalyzes the conversion ...

*Gi alpha subunit

The following G protein-coupled receptors couple to the Gi subunit: Acetylcholine M2 & M4 receptors Adenosine A1 & A3 receptors ... sst5 receptors Trace amine-associated receptor 8 Gi mainly inhibits the cAMP dependent pathway by inhibiting adenylate cyclase ... Therefore, the ultimate effect of Gi is the opposite of cAMP-dependent protein kinase. It is also attributed a minor role in ... α2C receptors Apelin receptors Calcium-sensing receptor Cannabinoid receptors (CB1 and CB2) Chemokine CXCR4 receptor Dopamine ...

*Neuromedin B

This receptor is a G protein-coupled receptor with seven transmembrane spanning regions, hence the receptor is also denoted as ... The free G-α iactivates adenylate cyclase (AC), which, in turn, catalyzes the conversion of ATP to cAMP, the latter of which ... cAMP activates of the enzyme Protein Kinase A (PKA). PKA enters the nucleus and activates the cAMP response element-binding ... the heterotrimeric G protein that is attached to the receptor is activated. The G-protein is called heterotrimeric because it ...

*Adrenergic agonist

... α2 receptors inhibit adenylate cyclase (via Gi), decreasing the activity of protein kinase A (PKA); β receptors activate ... All adrenergic receptors are G-protein coupled, activating signal transduction pathways. The G-protein receptor can affect the ... α1 receptors activate phospholipase C (via Gq), increasing the activity of protein kinase C (PKC); ... The receptors are broadly grouped into α and β receptors. There are two subclasses of α-receptor, α1 and α2 which are further ...

*Gs alpha subunit

Adenylate Cyclase stimulator). The G protein-coupled receptors that couple to this kind of G-protein include: 5-HT receptors ... in turn activates cAMP-dependent protein kinase. Further effects of Gs are thus found in function of cAMP-dependent protein ... receptor 1 Prostaglandin receptor types D2 and I2 Secretin receptor Thyrotropin receptor Trace amine-associated receptor 1 The ... FSH-receptor Gastric inhibitory polypeptide receptor Glucagon receptor Growth-hormone-releasing hormone receptor Histamine H2 ...

*Metabotropic glutamate receptor

"Metabotropic glutamate receptors negatively coupled to adenylate cyclase inhibit N-methyl-D-aspartate receptor activity and ... acting as a cofactor for the activation of protein kinase C. These receptors are also associated with Na+ and K+ channels. ... They are members of the group C family of G-protein-coupled receptors, or GPCRs. Like all glutamate receptors, mGluRs bind with ... by activating a G protein that inhibits the enzyme adenylyl cyclase, which forms cAMP from ATP. These receptors are involved in ...

*Opioid receptor

Opioid receptors are a type of G protein-coupled receptor (GPCR). These receptors are distributed throughout the central ... This includes inhibiting neuronal adenylate cyclase activity, as well as increasing membrane hyper-polarisation. When the ... cAMP binds to, and activates cAMP-dependant protein kinase A (PKA), which is located intracellularly in the neuron. The PKA ... Opioid receptors are a group of inhibitory G protein-coupled receptors with opioids as ligands. The endogenous opioids are ...

*Olfactory receptor neuron

The activated OR in turn activates the intracellular G-protein, GOLF (GNAL), adenylate cyclase and production of cyclic AMP ( ... The surface of these cilia is covered with olfactory receptors, a type of G protein-coupled receptor. Each olfactory receptor ... "Phosphorylation and inhibition of olfactory adenylyl cyclase by CaM kinase II in Neurons: a mechanism for attenuation of ... but many separate olfactory receptor cells express ORs which bind the same set of odors. The axons of olfactory receptor cells ...
Ca2 Influx and Tyrosine Kinases Trigger Bordetella Adenylate Cyclase Toxin ACT Endocytosis. Cell Physiology and Expression of the CD11b-CD18 Integrin Major Determinants of the Entry Route. . Biblioteca virtual para leer y descargar libros, documentos, trabajos y tesis universitarias en PDF. Material universiario, documentación y tareas realizadas por universitarios en nuestra biblioteca. Para descargar gratis y para leer online.
The adenylate cyclase toxin (AC toxin) is necessary for disease caused by Bordetella pertussis, which has reemerged in the United States over the last two decad...
The effects of Ca2+-calmodulin on adenylate cyclase activity in EGTA-washed, 27000 g particulate fractions of mouse and rat pancreatic islets were studied. Ca2+ (10 microM)-calmodulin (1 microM) stimulated adenylate cyclase activity 53.1 +/- 5.2 (N = 6)% in the particulate fraction of rat islets. Trifluoperazine (50 microM), a specific inhibitor of calmodulin, inhibited the Ca2+-calmodulin activation of the adenylate cyclase activity of this fraction of rat islets. These results confirm previous reports dealing with Ca2+-Calmodulin and rat islet adenylate cyclase [Valverde, Vandermeers. Anjaneyulu & Malaisse (1979) Science 206, 225-227; Sharp, Wiedenkeller, Kaelin, Siegel & Wollheim (1980) Diabetes 29, 74-77]. In contrast, however, Ca2+ (1-100 microM)-calmodulin (1-10 microM) did not stimulate the adenylate cyclase activity in the ...
Inositol phosphate accumulation and adenylate cyclase activity were investigated in the cortex of young and aged ethanol-treated rats. Three months of ethanol treatment of young rats decreased maximal stimulation of inositol phosphate accumulation by carbachol by 26%, from 494 ± 76% of basal turnover in control animals to 396 ± 54% in ethanol-treated animals (mean ± SD). In aged rats ethanol-related changes were no longer observed but age-related changes were evident. EC50 was significantly higher than in young animals and maximal stimulation was significantly lower. Basal adenylate cyclase activity in cortical membranes of all groups of animals was not different. Forskolin-stimulated adenylate cyclase activity was not affected by ethanol treatment, but was higher in aged animals. The activity of forskolin-stimulated adenylate cyclase in the presence of carbachol was higher ...
Bordetella pertussis adenylate cyclase. Penetration into host cells.: Exposure of Chinese hamster ovary, mouse adrenal cortex tumor (Y-1), THP-1 and U-937 cells
TY - JOUR. T1 - Hormone-sensitive adenylate cyclase in glomerular cells. Possible role for inflammatory diseases of the glomerulus. AU - Paietta, Elisabeth M.. AU - Schwarzmeier, J. D.. AU - Simbruner, G.. AU - Latzka, U.. AU - Lubec, G.. PY - 1981. Y1 - 1981. N2 - Using the adenylate cyclase assay after Ross the authors examined hormone sensitivity of isolated glomerular cells. cAMP production was increased 1.3-1.6-fold by stimulation with isoproterenol, 1.5-1.8 times by prostaglandin E 1 and 1.4-1.5 times by histamine. The isoproterenol reaction could be completely inhibited by propranolol, the histamine effect was abolished by the H2-blocking agent cimetidine. As a control the authors applied sodium fluoride, which directly activates the catalytic adenylate cyclase unit, increasing the activity 1.8-2.7 times (depending on the method of homogenization). These findings could reflect some physiological or ...
1. Sepharose 6B gel-filtration analysis of soluble adenylate cyclase from bovine corpus luteum is described. Both zonal and frontal techniques of analysis were used. 2. Under conditions of zonal analysis recoveries of activity were low. It was concluded that dissociation of two or more components of the adenylate cyclase complex was occurring on the column and that the maintenance of the complex was essential for the high-activity state of the catalytic unit. Two peaks of adenylate cyclase activity, of approximate mol. wts. 45,000 and 160,000 were detected. 3. The theory of frontal analysis (or steady-state gel filtration), applied to the study of the interacting components of the adenylate cyclase complex is discussed, and activity profiles are predicted. Activity profiles obtained experimentally be frontal analysis compared well with the theoretically predicted profile and ...
The effect of exogenously added adenylate cyclase from Bordetella pertussis (strain 114) has been investigated in Y-1 mouse adrenal tumor, chinese hamster ovary (CHO) and several other cells. A partially purified adenylate cyclase was found not to enter cells but, nevertheless, produced large amounts of cAMP in the medium. We could show that this resulted from release of ATP (and not larger molecules). The ATP released by the cells could be (1) directly measured and was replenished after each change of medium; (2) was reciprocally related to the cAMP produced; and (3) was competed for by ATPases present in added serum or by hexokinase and, less effectively, by exoenzymes on the cell surface. The extent of ATP leakage varied widely between different cell lines, being marked in CHO and Y-1 adrenal cells but negligible in transformed lymphocyte lines. The uncertainty of the origin of cAMP found in media of cultured cells requires separate ...
Adenylate cyclase toxin (CyaA) from Bordetella pertussis can subvert host immune responses allowing bacterial colonization. Here we have examined its adjuvant and immunomodulatory properties and the possible contribution of lipopolysaccharide (LPS), known to be present in purified CyaA preparations. CyaA enhanced antigen-specific interleukin-5 (IL-5) and IL-10 production and immunoglobulin G1 antibodies to coadministered antigen in vivo. Antigen-specific CD4+-T-cell clones generated from mice immunized with antigen and CyaA had cytokine profiles characteristic of Th2 or type 1 regulatory T (Tr1) cells. Since innate immune cells direct the induction of T-cell subtypes, we examined the influence of CyaA on activation of dendritic cells (DC) and macrophages. CyaA significantly augmented LPS-induced IL-6 and IL-10 and inhibited LPS-driven tumor necrosis factor alpha and IL-12p70 production from bone marrow-derived DC and macrophages. CyaA also enhanced cell surface expression of ...
A factor [the feedback regulator (FR)] formed by adipocytes after the stimulation of a cAMP raising hormone has been found to be a potent inhibitor of membrane-bound adenylate cyclase [EC 4.6.1.1.; ATP pyrophosphate-lyase (cyclizing)]. In a standard assay system using rat adipocyte plasma membrane as the source of adenylate cyclase, the FR inhibited adenylate cyclase by lowering the Vmax without affecting the apparent Km for ATP (0.3-0.6 mM). The apparent Ka for epinephrine (5-6 muM) was also not affected by FR. The inhibitory action of FR was partially countered by Mg2+ ions. An increase in phosphorylation of plasma membrane was observed when FR was present in the incubation system. The concentration required for a 50% inhibition was four times higher when adenosine 5-(beta,gamma-imino) triphosphate [AMP-P(NH)P] replaced ATP as the substrate for adenylate cyclase, implying ...
TY - JOUR. T1 - Multiple forms of brain adenylate cyclase. T2 - Stimulation by Mn2+. AU - Malamuda, Daniel F.. AU - DiRusso, Concetta C.. AU - Aprille, June R.. PY - 1977/11/23. Y1 - 1977/11/23. N2 - Mn2+-stimulated adenylate cyclase (ATP pyrophosphate-lyase-(cyclizing), EC 4.6.1.1) activity in detergent solubilized preparations from mouse brain. While NaF-stimulated activity was decreased by both solubilization and storage at 0-4°C, the ability of the enzyme to be stimulated by Mn2+ was maintained for up to one week. By including Mn+ in the assay of adenylate cyclase in gel fractions after isoelectric focusing, two distinct peaks of enzyme activity (pI1 = 5.8, pI2 = 6.4) were detected, suggesting the existence of more than one type of catalytic subunit in mouse brain cell membranes.. AB - Mn2+-stimulated adenylate cyclase (ATP pyrophosphate-lyase-(cyclizing), EC 4.6.1.1) ...
Aiba H.. The regulatory region of the Escherichia coli cya gene was analyzed by using S1 nuclease mapping and in vitro transcription experiments. The cya gene was transcribed, both in vivo and in vitro, from one major promoter (P2) and two weak promoters (P1 and P1) that are located about 200 base pairs upstream of P2. The transcription from P2 was specifically inhibited by cAMP-CRP (cAMP receptor protein) in vitro. This regulatory mechanism was shown to be physiologically relevant through quantitative analyses of the cya mRNA in intact cells by S1 and dot blot assays. DNase I protection experiments revealed that cAMP-CRP binds to the cya DNA region between +11 and -20, in which a consensus CRP binding sequence is present. Moreover, it was found that cAMP-CRP alters the binding of RNA polymerase to the promoter region, thus inhibiting the transcription of the cya gene.. J. Biol. Chem. 260:3063-3070(1985) [PubMed] [Europe PMC] ...
BioAssay record AID 41661 submitted by ChEMBL: Beta-3 agonist efficacy in an adenylate cyclase assay performed on chinese hamster ovary cells transfected with human Beta-3 adrenergic receptor; Inactive.
We next investigated whether beta gamma subunits play a role in the sensitization of type VI adenylyl cyclase activity; using expression of alpha tau to inhibit beta gamma-mediated effects, we found that the quinpirole-induced sensitization of type VI adenylyl cyclase was abolished ...
Attenuation of inhibitory influence of hormones on adenylyl cyclase systems in the myocardium and brain of obese and type 2 diabetic rats as affected by the intranasal insulin treatment Journal of Evolutionary Biochemistry and Physiology Pleiades Publishing 0022-0930 1608-3202 10.1134/S0022093014050044
Vaccines designed to stimulate CTL should be able to deliver protein antigens to the cytoplasm of host cells for processing and presentation by MHC-I. Many systems have been exploited to accomplish cytoplasmic delivery, including viral and bacterial vectors and DNA vaccines (7, 8, 14, 22, 27, 33, 36). There have also been reports demonstrating that antiviral immunity can be primed in mice vaccinated with a recombinant Bordetella adenylate cyclase toxin incorporating a CTL epitope from LCMV (11, 29, 31); however, the data demonstrated protection only when the recombinant toxin was injected in the presence of an adjuvant, aluminum hydroxide (29). Therefore, it remains unclear whether the antiviral protection was a result of toxin delivery or adjuvant activity. This report describes the use of a nontoxic, truncated form of anthrax toxin as an epitope delivery system without the use of adjuvant.. We demonstrate that protective immunity against a viral pathogen, ...
Serotonin and dopamine stimulate distinct postsynaptic sensitive adenylate cyclases in homogenates of various brain areas in newborn rats [Enjalbert, A., Bourgoin, S., Hamon, M., Adrien, J. & Bockaert, J. (1978) Mol. Pharmacol., 14, 000-000]. However, maximal effects of dopamine and serotonin on the adenylate cyclase activity in the striatum and the hypothalamus were not strictly additive. In fact, in striatum serotonin inhibited the dopamine-sensitive adenylate cyclase noncompetitively. Conversely, the maximal effects of serotonin and l-isoproterenol (a pure beta adrenergic agonist) on adenylate cyclase activity in homogenates of the cerebral cortex were strictly additive. Classical serotoninergic agonists [D-lysergic acid diethylamide (LSD), bufotenine, 5-methoxy-N,N-dimethyltryptamine] activated the adenylate cyclase in collicular ...
The enzyme soluble adenylyl cyclase (sAC) is directly stimulated by bicarbonate (HCO3−) to produce the signaling molecule cyclic adenosine monophosphate (cAMP). Because sAC and sAC‐related enzymes are found throughout phyla from cyanobacteria to mammals and they regulate cell physiology in response to internal and external changes in pH, CO2, and HCO3−, sAC is deemed an evolutionarily conserved acid‐base sensor. Previously, sAC has been reported in dogfish shark and round ray gill cells, where they sense and counteract blood alkalosis by regulating the activity of V‐type H+‐ ATPase. Here, we report the presence of sAC protein in gill, rectal gland, cornea, intestine, white muscle, and heart of leopard shark Triakis semifasciata. Co‐expression of sAC with transmembrane adenylyl cyclases supports the presence of cAMP signaling microdomains. Furthermore, immunohistochemistry on tissue sections, and western blots and cAMP‐activity assays on nucleus‐enriched ...
The interaction of the renin-angiotensin system and the sympathetic nervous system in patients with congestive heart failure is not well understood. We tested the hypothesis that angiotensin-converting enzyme inhibitors can resensitize the beta-adrenergic receptor system. Guinea pigs were given captopril, isoproterenol, or both for 2 weeks. At death, cardiac sarcolemmal and light vesicle fractions and intact mononuclear leukocytes were prepared. Captopril treatment led to an up-regulation of cardiac beta 1- but not mononuclear leukocyte beta 2-adrenergic receptors and an increase in isoproterenol-stimulated adenylate cyclase activity in the heart. Animals treated with isoproterenol developed cardiac hypertrophy, had increased plasma norepinephrine levels, and had a decreased number and responsiveness of both cardiac and mononuclear leukocyte beta-adrenergic receptors. Concomitant treatment with captopril attenuated ...
Purified sarcolemmal and light vesicle (intracellular) fractions of beta-adrenergic receptors were used to examine the effects of propranolol on receptor translocation in guinea pig heart. Guinea pigs were given propranolol (0.15 mg/kg/hr) via minipumps for 7 days and either killed or made ischemic for 1 hour via a coronary ligature. Propranolol treatment led to an externalization of beta-receptors from light vesicle to sarcolemmal fractions. This externalization increased the number of surface beta-adrenergic receptors that were functional, as assessed by isoproterenol-stimulated adenylate cyclase activity. After chronic propranolol treatment, ischemia did not further alter receptor distribution. These results suggest that externalization of beta-adrenergic receptors from a light vesicle fraction to the sarcolemma contributes to up-regulation of ...
Pertussis, also known as whooping cough, is an acute respiratory infectious disease caused by a bacteria called Bordetella Pertussis. The characteristic symptoms are paroxysmal cough, inspiratory wheezing and post-tussive vomiting. Following the inhalation of respiratory secretions from an infected individual, bacteria enter the upper respiratory tract and adhere to epithelial cells. Several adhesion factors have been implicated: the filamentous hemagglutinin (FHA), fimbriae, and pertactin (Prn). Pertussis toxin (Ptx) and adenylate cyclase toxin (ACT) have been identified so far as major protein toxins of B. pertussis. PTX is a hexameric AB5-type exotoxin. Catalytic A subunit catalyzes the ADP-ribosylation of the Gi subunits of the heterotrimeric G protein, then inhibits multiple downstream pathways. ACT is able to penetrate the cytoplasmic membrane of host cells and becomes activated through the cleavage and the binding of calmodulin (CaM). ...
Adrenocorticotropin/α-melanocyte-stimulating hormone (ACTH/MSH)-like peptides modulate adenylate cyclase activity in rat brain slices: evidence for an ACTH/MSH receptor-coupled ...
Treatment of rats with chemical carcinogens, including 2-acetylaminofluorene (2-AAF), leads to a strong increase in the hepatic catecholamine-sensitive adenylate cyclase activity. The present study was undertaken to investigate the mechanism for the development of this increase. We report that hepatocytes isolated from rats which had been fed 2-AAF (0.025% w/w) for 8-12 weeks had an increased number of β-adrenoceptors, as determined by [3H]dihydroalprenolol binding to whole cells and [125I]iodocyanopindolol binding to washed particles. For both ligands the number of binding sites was about 4-fold higher in hepatocytes from 2-AAF-treated rats than in those from controls. The adenylate cyclase activity of the carcinogen-fed animals showed both a general increase manifested in the basal level (2-fold) and in the activities obtained by stimulation with guanine nucleotides (2-3-fold), cholera toxin (1.5-fold), and glucagon (1.3-fold) and a ...
At present, divergent views exist concerning the extent to which either opioid receptor desensitization or adenylate cyclase superactivation contribute to the development of tolerance to morphine. The receptor activity versus endocytosis (RAVE) model proposes that morphine may induce adenylate cyclase superactivation to a greater extent than other opioids, which in turn exacerbates the development of tolerance (Whistler et al, 1999; Finn and Whistler, 2001). In contrast, studies using mice lacking β‐arrestin‐2 show that opioid receptor desensitization directly contributes to tolerance and that tolerance and adenylyl cyclase superactivation are two dissociable phenomena (Bohn et al, 1999, 2000). Here, we propose that morphine is unique in that it promotes terminal opioid receptor desensitization by inducing a sustained phosphorylation of Ser375. ...
Efficient gene transfer by vectors that can be easily delivered to target organs is desirable in clinical gene therapy. We tested the hypothesis that intracoronary infusion of the nitric oxide donor nitroprusside would increase the efficiency of adenovirus vector-mediated gene transfer to the heart. Intracoronary delivery of an adenovirus encoding murine adenylyl cyclase type VI (Ad.AC(VI)) was performed in adult pigs with and without simultaneous intracoronary infusion of nitroprusside. Animals were killed 12-14 days after Ad.AC(VI) delivery and myocardial adenylyl cyclase activity was measured. Addition of nitroprusside during intracoronary infusion of Ad.AC(VI) was associated with a 4-fold increase in cAMP-generating capacity in the left ventricle. Transgene expression was confirmed by immunoblotting. Intracoronary nitroprusside produced mild dose-dependent changes in blood pressure and heart rate during infusion. Intracoronary nitroprusside infusion is a safe and ...
TY - JOUR. T1 - Adenylyl cyclases in the digestive system. AU - Sabbatini, Maria Eugenia. AU - Gorelick, Fred. AU - Glaser, Shannon. PY - 2014/1/1. Y1 - 2014/1/1. N2 - Adenylyl cyclases (ACs) are a group of widely distributed enzymes whose functions are very diverse. There are nine known transmembrane AC isoforms activated by Gαs. Each has its own pattern of expression in the digestive system and differential regulation of function by Ca2+ and other intracellular signals. In addition to the transmembrane isoforms, one AC is soluble and exhibits distinct regulation. In this review, the basic structure, regulation and physiological roles of ACs in the digestive system are discussed.. AB - Adenylyl cyclases (ACs) are a group of widely distributed enzymes whose functions are very diverse. There are nine known transmembrane AC isoforms activated by Gαs. Each has its own pattern of expression in the digestive system and differential regulation of function by Ca2+ ...
Recently Peeters and colleagues (2006) discovered a mechanism in yeast by which the G alfa protein Gpa2 activates PKA through two kelch-repeat proteins, Krh1 and Krh2, bypassing adenylate cyclase stimulation. Hence, Gpa2 regulates PKA activity via two distinct pathways: through stimulation of adenylate cyclase and through inhibition of the Krh proteins. We investigated if the C. glabrata homologues of ScKrh1 and ScKrh2 can complement the respective deletion mutants of S. cerevisiae. By measuring the trehalose content of the respective deletions mutants, transformed with CgKrh1 and CgKrh2 cloned into pBEVY-vectors, after 12, 24 and 48 hours, we showed that ChKrh1 and ChKrh2 can complement the function of ScKrh1 and ScKrh2. We will also investigate the expression of STRE-controlled genes and the formation of pseudohyphae in these transformed deletion mutants ...
RecName: Full=Adenylate cyclase type 3; EC=4.6.1.1;AltName: Full=Adenylate cyclase type III; Short=AC-III;AltName: Full=ATP pyrophosphate-lyase 3;AltName: Full=Adenylyl cyclase 3; Short=AC3;AltName: Full=Adenylate cyclase, olfactive type ...
METHODS AND RESULTS We examined the beta-adrenergic receptor-responsive adenylyl cyclase pathway in hearts from pigs subjected to volume-overload hypertrophy with circulatory congestion. Nine pigs underwent initial pharmacological and hemodynamic studies, and, 5 weeks after aortocaval fistula placement, when signs of circulatory congestion were evident, these measurements were repeated. Biochemical analyses of plasma and myocardium from these animals and seven normal animals were compared. Experimental animals showed signs of circulatory congestion (tachypnea, weight gain, pulmonary rales) within 3-4 weeks of fistula placement. Necropsy showed ascites and biventricular cardiac hypertrophy, but no fibrosis or inflammation was present on histological inspection. Heart rate responsiveness to beta AR stimulation was blunted, with ED50, for isoproterenol increased 133% (p less than 0.001) after development of circulatory congestion. Biochemical analyses of the beta AR-responsive ...
RecName: Full=Adenylate cyclase type 1; EC=4.6.1.1;AltName: Full=Adenylate cyclase type I;AltName: Full=ATP pyrophosphate-lyase 1;AltName: Full=Adenylyl cyclase 1;AltName: Full=Ca(2+)/calmodulin-activated adenylyl ...
Amphetamine has complex behavioral actions in the rat that depend upon the release of dopamine in striatal and mesolimbic brain regions. To explore a possible role of the dopamine-sensitive cAMP second-messenger system in mediating these effects, we examined the effects of in vivo amphetamine treatments on the D1 receptor-coupled adenylate cyclase system in membranes from striatal and mesolimbic rat brain regions. The results show that amphetamine produces a regional, dose- and time- dependent down-regulation of adenylate cyclase activity. Intermediate and high doses of amphetamine (2.5 and 7.5 mg/kg, respectively), but not a low dose (1.0 mg/kg), resulted in a decrease in the apparent Vmax and/or an increase in the apparent Ka for the selective D1 partial agonist, SKF38393, in striatal membranes 30 min after amphetamine treatment. Treatment of rats with 7.5 mg/kg amphetamine for 30 and 60 min, but not 10 ...
The beta 2-adrenergic transmembrane signal transduction was investigated in malignant B-cells from 15 patients with low grade non-Hodgkins lymphoma as compared with normal lymphocytes of seven healthy adults. The number of beta 2-adrenoceptors and the response of adenylate cyclase (AC) to isoproterenol were slightly decreased in lymphoma cells. The responsiveness of AC to forskolin was 8-fold lower in lymphoma cells, whereas the response to cholera toxin showed no difference. These findings demonstrate an impairment of the beta 2-adrenergic signal transduction in low grade lymphoma cells that particularly affects the function of AC. The comparison with forskolin resistant mutants of an adrenocortical tumor cell line, Y1 (Schimmer et al., J Biol Chem 262: 15521-15526, 1987), suggests that the availability of functional active alpha subunits of stimulatory G proteins (Gs) might be reduced in human B-cell lymphoma, although other mechanisms known to inhibit the ...
Macromolecule FORMYCIN-5-MONOPHOSPHATE C 1 0 H 1 4 N 5 O 7 P PBAHXXBYQACZMA-KSYZLYKTSA-N The hypoxanthine phosphoribosyltransferase (HPRT) from Trypanosoma cruzi, etiologic agent of Chagas disease, was cocrystallized with the inosine analogue Formycin B 1NC3: Structure of Escherichia coli 5-methylthioadenosine/ S-adenosylhomocysteine nucleosidase inhibitor complexes provide insight into the conformational changes Previous article in issue: 2-Methylene-3-quinuclidinone and its derivatives Previous article in issue: 2-Methylene-3-quinuclidinone and its derivatives Next article Abstract. Biochemistry. , Townsend, L. K. About DrugBank; Wishart Research Group; Structure, properties, spectra, suppliers and links for: formycin A, 6742-12-7. Formycin 5-triphosphate (FoTP), a fluorescent analog of ATP, is shown to be a substrate for the membrane-bound adenylate cyclase . Synonyms: Not Acetyldigitoxin may decrease the cardiotoxic activities of Formycin. Crystal structure of formycin ...
Signs of Multiple endocrine abnormalities - adenylyl cyclase dysfunction including medical signs and symptoms of Multiple endocrine abnormalities - adenylyl cyclase dysfunction, symptoms, misdiagnosis, tests, common medical issues, duration, and the correct diagnosis for Multiple endocrine abnormalities - adenylyl cyclase dysfunction signs or Multiple endocrine abnormalities - adenylyl cyclase dysfunction symptoms.
and forskolin-stimulated AC activity is increased by caveolin-1 knockdown or knockout, the results suggest that noninvolvement of Gαi or a GPCR coupled to Gαi. Alternatively, because caveolin-1 is a cholesterol-binding protein (Murata et al., 1995), limiting its expression could lower membrane cholesterol. This is not the case (Fig. 5). In fact, incubating wild-type or Cav-1 RNAi cells with 1 mg/ml exogenous cholesterol significantly decreased isoproterenol-stimulated cAMP accumulation (Fig. 5). Thus, removing membrane cholesterol does seem to enhance βAR/Gαs/adenylyl cyclase signaling (most likely by disrupting rafts/caveolae), and adding cholesterol has the opposite effect. Therefore, the elevated cAMP signaling due to loss of caveolin is independent of Gαi and cholesterol levels.. Lipid rafts/caveolae can influence both spatial organization at the membrane and intracellular trafficking of signaling molecules; both mechanisms could regulate the ...
This study was performed to investigate the regulatory mechanism of cerebral blood flow of adenosine A $_{2B}$ receptor agonist in the rats, and to define whether its mechanism is mediated by adenylate cyclase, guanylate cyclase and potassium channel. In pentobarbital-anesthetized, pancuronium-par...
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B pertussis produces numerous virulence factors, including toxins and attachment agents, many of which are antigenic and included in the acellular vaccine. The link of each virulence factor to clinical illness has been difficult to elucidate due to lack of an animal model for experimentation. However, a recently developed model in infant baboons has the potential to address unanswered questions. The bacteria attach to ciliated epithelial cells of the respiratory tract, induce ciliary paralysis and local inflammation, and thicken and decrease clearance of secretions. B pertussis is not invasive. Pertussis toxin, necessary but not sufficient to cause clinical pertussis, is secreted by the bacteria and affects G-protein function, which prevents migration of lymphocytes to the area of infection, and inhibits the function of neutrophils, macrophages, monocytes, and lymphocytes. Adenylate cyclase toxin invades phagocytes and induces high levels of cyclic adenosine ...
Sesquiterpene cyclase, a branch point enzyme in the general isoprenoid pathway for the synthesis of phytoalexin capsidiol, was induced in detached leaves of Capsicum annuum (pepper) by UV treatment. The inducibility of cyclase enzyme activities paralleled the absolute amount of cyclase protein(s) of pepper immunodetected by monoclonal antibodies raised against tobacco sesquiterpene cyclase. A cDNA library was constructed with poly(A)+ RNA isolated from 24 h UV-challenged leaves of pepper. A cDNA clone for sesquiterpene cyclase in pepper was isolated by using a tobacco 5-epi aristolochene synthase gene as a hetero-logous probe. The predicted protein encoded by this cDNA was comprised of 559 amino acids and had a relative molecular mass of 65,095. The primary structural information from the cDNA clone revealed that it shared 77%, 72% and 49% identity with 5-epi aristolochene, vetispiradiene, ...
Little is known about the active site of guanylate cyclase, although it is assigned to a 239-amino acid region (catalytic domain).4 Since the catalytic domain of guanylate cyclase (GC-c) can be functionally expressed as a soluble protein in E coli, it, rather than the whole enzyme, may be an ideal system for studying the active site of guanylate cyclase. Using guanylate cyclase assay, we screened several PCR-cloned gene products of GC-c and identified a mutant that lacks enzyme activity. Results of cDNA sequencing revealed that Leu 817 is converted into an Arg residue in the mutant. Sequence comparison reveals that Leu 817 is conserved in the corresponding position of most known guanylate cyclases and adenylate cyclases. These results suggest that Leu 817 of guanylate cyclase may play an important functional or structural role.. GC-A has been reported to ...
BACKGROUND: Cholera toxin produces intestinal secretion by activation of the adenylate cyclase complex. However animal studies have shown 5-hydroxytryptamine may be released after exposure to cholera toxin, and thereby contribute to the secretory state. AIM: To determine whether cholera toxin releases 5-hydroxytryptamine in human jejunum. SUBJECTS: Seven male subjects were given a subclinical dose of cholera toxin in a paired, controlled, randomised, double blind study. METHODS: A closed 10 cm segment of upper jejunum was exposed to 15 micrograms of cholera toxin for two hours prior to closed segment perfusion with plasma electrolyte solution containing a non-absorbable volume marker, [14C]-polyethylene glycol. 5-Hydroxytryptamine in jejunal effluent and 5-hydroxyindoleacetic acid in urine (up to seven hours after cholera toxin) were measured by high performance liquid chromatography with fluorimetric detection. RESULTS: In contrast with controls, all subjects secreted fluid ...
Adipocytes of hypothyroid rats display an increased responsiveness to agents which function by inhibiting the production of cyclic AMP. Anti-peptide antisera which selectively recognise the alpha subunit of the inhibitory guanine nucleotide binding protein (Gi) detected a 40 kDa polypeptide in adipocyte plasma membranes of both euthyroid and hypothyroid rats. Amounts of the alpha subunit of Gi were elevated some 2-fold in the hypothyroid preparations in comparison with the euthyroid controls, when equal amounts of membrane protein of the two treatments were examined. As cells from the hypothyroid animals contained 2.7 times as much membrane protein as those from the control animals, the amounts of alpha subunit of Gi are elevated some 5.6-fold per cell in adipocytes of the hypothyroid animals compared with the euthyroid controls. Amounts of the 36 kDa beta subunit of G-proteins were also elevated in plasma membranes of adipocytes of ...
This study investigates the hypothesis that inflammatory cytokines, interleukin (IL)-1alpha IL-1beta, and tumor necrosis factor (TNF), influence cardiac function by affecting calcium homeostasis and that this effect is mediated by the beta-adrenergic-adenylate cyclase system. After 4 days in culture, neonatal rat ventricular myocytes were treated with cytokines (10 ng/ml) for short (2 h) or longer (18 h) times. Myocyte calcium, contractility, and adenylate cyclase were measured under each condition. Anticipated stepwise increases in adenylate cyclase and intracellular calcium were found in controls (non-cytokine-treated) with 10(-7) M isoproterenol, 10(-7) M isoproterenol + 0.1 mM guanosine triphosphate, and 10(-9) M forskolin. Cells in the presence of cytokine for 2 h show increased basal calcium levels but no changes in adenylate cyclase activities, and isoproterenol fails ...
In this study, the ability of a series of dynorphin peptides to inhibit adenylyl cyclase (AC) activity was determined. The endogenous ligand of the kappa opioid receptor, dynorphin A(l-17) (Dyn A(l-17)), produced a significant concentration-dependent inhibition of AC activity in membranes prepared from the caudate putamen (CPu) of naive Fischer 344 rats. The opioid receptor antagonist, naloxone (10(-5)M), which is predominantly mu opioid receptor directed, but with modest kappa and delta receptor activity, partially blocked this inhibition. Nor-Binaltorphimine (10(-5)M), the selective kappa receptor antagonist, also blocked the effect of Dyn A(l-17), but to a lesser degree. [Des-Tyr1]Dyn A(2-17), a major nonopioid biotransformation product of Dyn A(l-17) with known biological activities, also inhibited AC in rat CPu membranes. Dyn A(l-13) inhibited AC, as did its major opioid biotransformation product, Dyn ...
The present study was carried out to determine, first, the cardiac beta -adrenergic receptor characteristics of normal chickens and chickens with heart failure and, second, the characteristics of myocardial beta -adrenergic receptors in non-hypertrophied hearts in broilers exposed to two different altitude and temperature programmes. The density of beta -adrenergic receptors was significantly lower in myocardial cells in right ventricular failure birds compared with healthy birds. The binding capacity of beta -adrenergic receptors was reduced in the non-hypertrophied ventricles after exposure to high altitude in the younger but not in older chickens. At both altitudes, beta -adrenergic receptor binding capacity was not significantly different in low temperature compared with normal temperature birds. These data support the hypothesis of beta -adrenergic receptor downregulation as one of the mechanisms of ...
α-Melanocyte-Stimulating Hormone (MSH), amide stimulates melanocortin 1 receptor that results in the activation of adenylyl cyclase. - Mechanism of Action & Protocol.
TY - JOUR. T1 - Stress increases putative gonadotropin inhibitory hormone and decreases luteinizing hormone in male rats. AU - Kirby, Elizabeth D.. AU - Geraghty, Anna C.. AU - Ubuka, Takayoshi. AU - Bentley, George E.. AU - Kaufer, Daniela. PY - 2009/7/7. Y1 - 2009/7/7. N2 - The subjective experience of stress leads to reproductive dysfunction in many species, including rodents and humans. Stress effects on reproduction result from multilevel interactions between the hormonal stress response system, i.e., the hypothalamic-pituitary-adrenal (HPA) axis, and the hormonal reproductive system, i.e., the hypothalamic-pituitary-gonadal (HPG) axis. A novel negative regulator of the HPG axis known as gonadotropin-inhibitory hormone (GnIH) was recently discovered in quail, and orthologous neuropeptides known as RFamide-related peptides (RFRPs) have also been identified in rodents and primates. It is currently unknown, however, whether GnIH/RFRPs influence HPG axis activity in response to stress. We show ...
Vasoactive intestinal peptide receptor 2 also known as VPAC2, is a G-protein coupled receptor that in humans is encoded by the VIPR2 gene. VIPR2 is expressed in the uterus, prostate, smooth muscle of the gastrointestinal tract, seminal vesicles and skin, blood vessels and thymus. VIPR2 is also expressed in the cerebellum. Vasoactive intestinal peptide (VIP) and pituitary adenylate cyclase activating polypeptide (PACAP) are homologous peptides that function as neurotransmitters and neuroendocrine hormones. While the receptors for VIP (VIRP 1 and 2) and PACAP (ADCYAP1R1) share homology, they differ in their substrate specificities and expression patterns. VIPR2 transduction results in upregulation of adenylate cyclase activity. Furthermore, VIPR2 mediates the anti-inflammatory effects of VIP. Research using VPAC2 knockout mice implicate it in the function of ...
G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synthetic opioids and for the psychoactive diterpene salvinorin A. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling leads to the inhibition of adenylate cyclase activity. Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Plays a role in the perception of pain. Plays a role in mediating reduced physical activity upon treatment with synthetic opioids. Plays a role in the regulation of salivation in response to synthetic ...
Nestler EJ (August 2016). "Reflections on: "A general role for adaptations in G-Proteins and the cyclic AMP system in mediating the chronic actions of morphine and cocaine on neuronal function"". Brain Research. 1645: 71-4. doi:10.1016/j.brainres.2015.12.039. PMC 4927417. PMID 26740398. These findings led us to hypothesize that a concerted upregulation of the cAMP pathway is a general mechanism of opiate tolerance and dependence. ... We thus extended our hypothesis to suggest that, particularly within brain reward regions such as NAc, cAMP pathway upregulation represents a common mechanism of reward tolerance and dependence shared by several classes of drugs of abuse. Research since that time, by many laboratories, has provided substantial support for these hypotheses. Specifically, opiates in several CNS regions including NAc, and cocaine more selectively in NAc induce expression of certain adenylyl cyclase isoforms and PKA subunits via the transcription factor, CREB, and ...
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We have characterized the adenylyl cyclase activity in a newly developed preparation of isolated olfactory cilia from the bovine chemosensory neuroepithelium. Like its counterparts from frog and rat, the ciliary enzyme was stimulated by guanine nucleotides, by forskolin, and by a variety of odorants in the presence of GTP. The main difference between the bovine olfactory cilia preparation and the frog and rat olfactory cilia preparation is that odorant stimulation of the bovine olfactory adenylyl cyclase is strongly inhibited by submillimolar concentrations of dithiothreitol. This inhibition is a consequence of a concomitant increase in the GTP-stimulated level and the decrease of the odorant stimulation of the enzyme. Nasal respiratory cilia have a much lower level of adenylyl cyclase activity and show no odorant stimulation. Owing to the large quantities of material available, the bovine olfactory cilia preparation is advantageous for studies ...
Guanylate cyclase 2C, also known as guanylyl cyclase C (GC-C), intestinal guanylate cyclase, guanylate cyclase-C receptor, or the heat-stable enterotoxin receptor (hSTAR) is an enzyme that in humans is encoded by the GUCY2C gene. Guanylyl cyclase is an enzyme found in the luminal aspect of intestinal epithelium and dopamine neurons in the brain. The receptor has an extracellular ligand-binding domain, a single transmembrane region, a region with sequence similar to that of protein kinases, and a C-terminal guanylate cyclase domain. Tyrosine kinase activity mediates the GC-C signaling pathway within the cell. GC-C is a key receptor for heat-stable enterotoxins that are responsible for acute secretory diarrhea. Heat-stable enterotoxins are produced by pathogens such as Escherichia coli. Knockout mice deficient ...
In this study, using cAMP analogues, as well as the adenylate cyclase activator forskolin and the phosphodiesterase inhibitor, 3-isobutyl-1-methylxanthine, we have shown that cAMP potentiates cytokine induced iNOS activity, protein, and mRNA in the human intestinal epithelial cell line, DLD-1. Cyclic AMP has been shown to induce iNOS expression in many cell types but the majority of these are rat cell lines. Indeed, cAMP responsive element (CRE) sites have been identified in the rat iNOS gene39 and could be involved in the iNOS expression caused by cAMP alone or in combination with cytokines. Nevertheless, cAMP can also decrease iNOS expression in cells of rat origin.28 32 40 To our knowledge, only two studies have reported cAMP enhancement of iNOS expression in human cells, these being monocytes and T cells.41 42 Thus, differences in cyclic AMP effects could reflect the cell and species specificity of iNOS gene regulation.. As shown by northern blot ...
Metabotropic glutamate receptors (mGluRs) are coupled to effector systems through GTP-binding proteins (G-proteins) and appear to mediate slow synaptic responses in the CNS. Although mGluR-mediated increases in phosphoinositide hydrolysis have been well characterized, other mechanisms for signal transduction employed by mGluRs are poorly understood. We recently reported that the selective mGluR agonist 1- aminocyclopentane-1 S,3R-dicarboxylic acid (1S,3R-ACPD) increases cAMP accumulation in rat hippocampal slices. We have now investigated the mechanisms involved in this response. A number of G-protein-linked receptors that are not directly coupled to adenylate cyclase increase cAMP accumulation by potentiating cAMP responses to other agonists. Furthermore, previous studies suggest that glutamate increases cAMP accumulation by a mechanism that is dependent ...
hypothetical protein, 5-ht7, 5Ht7, 5-HT-7, 5-HT7 receptor, 5-HT receptor 7a, 5-HT-X, 5-hydroxytryptamine 7 receptor, 5-hydroxytryptamine7 receptor, 5-hydroxytryptamine (serotonin) receptor 7, 5-hydroxytryptamine (serotonin) receptor 7 (adenylate cyclase-coupled), 5-hydroxytryptamine (serotonin) receptor 7, adenylate cyclase-coupled, Anapl_03536, AS27_02610, AS28_04456, CB1_000689030, D623_10028851, GPRFO, H920_08680, high affinity serotonin receptor (5HT7), I79_004939, M91_18026, M959_09888, MDA_GLEAN10014860, N300_07498, N301_10640, N302_13493, N305_11464, N306_13870, N307_06146, N308_09036, N330_05281, N331_09625, N334_00682, PAL_GLEAN10018375, serotonin 5-hydroxytryptamine 7-a receptor, serotonin receptor 7, Y1Q_023580, ...
Guanyl nucleotide binding-proteins, or G-proteins, are ubiquitous molecules that are involved in cellular signal transduction mechanisms. Because a role has been established for cAMP in meiosis and G-proteins participate in cAMP-generating systems by stimulating or inhibiting adenylate cyclase, the present study was conducted to examine the possible involvement of G-proteins in the resumption of meiotic maturation. Cumulus cell-free mouse oocytes (denuded oocytes) were maintained in meiotic arrest in a transient and dose-dependent manner when microinjected with the nonhydrolyzable GTP analog, GTP gamma S. This effect was specific for GTP gamma S, because GppNHp, GTP, and ATP gamma S were without effect. Three compounds, known to interact with G-proteins, were tested for their ability to modulate meiotic maturation: pertussis toxin, cholera toxin, and aluminum fluoride (AlF4-). ...
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Mechanisms mediating the cardioprotective actions of glucagon-like peptide 1 (GLP-1) were unknown. Here, we show in both ex vivo and in vivo models of ischemic injury that treatment with GLP-1(28-36), a neutral endopeptidase-generated (NEP-generated) metabolite of GLP-1, was as cardioprotective as GLP-1 and was abolished by scrambling its amino acid sequence. GLP-1(28-36) enters human coronary artery endothelial cells (caECs) through macropinocytosis and acts directly on mouse and human coronary artery smooth muscle cells (caSMCs) and caECs, resulting in soluble adenylyl cyclase Adcy10-dependent (sAC-dependent) increases in cAMP, activation of protein kinase A, and cytoprotection from oxidative injury. GLP-1(28-36) modulates sAC by increasing intracellular ATP levels, with accompanying cAMP accumulation lost in sAC-/- cells. We identify mitochondrial trifunctional protein-α (MTPα) as a binding partner of GLP-1(28-36) and demonstrate that the ability of ...
Mechanisms mediating the cardioprotective actions of glucagon-like peptide 1 (GLP-1) were unknown. Here, we show in both ex vivo and in vivo models of ischemic injury that treatment with GLP-1(28-36), a neutral endopeptidase-generated (NEP-generated) metabolite of GLP-1, was as cardioprotective as GLP-1 and was abolished by scrambling its amino acid sequence. GLP-1(28-36) enters human coronary artery endothelial cells (caECs) through macropinocytosis and acts directly on mouse and human coronary artery smooth muscle cells (caSMCs) and caECs, resulting in soluble adenylyl cyclase Adcy10-dependent (sAC-dependent) increases in cAMP, activation of protein kinase A, and cytoprotection from oxidative injury. GLP-1(28-36) modulates sAC by increasing intracellular ATP levels, with accompanying cAMP accumulation lost in sAC-/- cells. We identify mitochondrial trifunctional protein-α (MTPα) as a binding partner of GLP-1(28-36) and demonstrate that the ability of ...
Previous studies on immortalized B lymphoblasts from patients with EH and enhanced Na+-H+ exchanger activity have revealed an enhanced activation of PTX-sensitive G proteins.7 This conclusion was mainly based on two findings. First, HT lymphoblasts displayed enhanced [Ca2+]i signals upon stimulation with platelet-activating factor and somatostatin. Pretreatment with PTX strongly reduced these agonist-evoked Ca2+ signals, and the residual Ca2+ responses were no longer different between NT and HT cell lines. Second, both receptor-mediated stimulation and direct (by mastoparan-7) stimulation of GTPγS binding to PTX-sensitive G proteins were significantly increased in HT lymphoblasts.7 Unfortunately, B lymphoblasts apparently do not express functional receptors that are selectively coupled to PTX-insensitive G proteins, eg, Gq or Gs. Therefore, our proposal of a selective enhancement of signal transduction via ...
Defects in phosphotransferase chemotaxis in cya and cpd mutants previously cited as evidence of a cyclic GMP or cyclic AMP intermediate in signal transduction were not reproduced in a study of chemotaxis in Escherichia coli and Salmonella typhimurium. In cya mutants, which lack adenylate cyclase, the addition of cyclic AMP was required for synthesis of proteins that were necessary for phosphotransferase transport and chemotaxis. However, the induced cells retained normal phosphotransferase chemotaxis after cyclic AMP was removed. Phosphotransferase chemotaxis was normal in a cpd mutant of S. typhimurium that has elevated levels of cyclic GMP and cyclic AMP. S. typhimurium crr mutants are deficient in enzyme III glucose, which is a component of the glucose transport system, and a regulator of adenylate cyclase. After preincubation with cyclic AMP, the crr mutants were deficient in enzyme II glucose-mediated transport and ...
TY - JOUR. T1 - Potentiated anaphylaxis in patients with drug-induced beta-adrenergic blockade. AU - Jacobs, Robert L.. AU - Rake, Geoffrey W.. AU - Fournier, Donald C.. AU - Chilton, Robert J. AU - Culver, William G.. AU - Beckmann, Charles H.. PY - 1981. Y1 - 1981. N2 - Anaphylaxis to known allergens occurred in two patients under treatment for hypertension with propranolol. The clinical course of both cases was similar. Bradycardia associated with an undetectable blood pressure, unusual severity, and sluggish response to treatment were major common factors in which blockade of the beta-adrenergic system may have had a role. Propranolol, a beta-adrenergic antagonist that acts competitively by blocking the adenylate cyclase receptor on efferent cells, is well recognized to cause increased airways resistance in some asthmatic and normal subjects. It is postulated that propranolol potentiated anaphylaxis in these patients by inhibition of ...
Background and purpose: Long-term morphine treatment enhances pain neurotransmitter (such as calcitonin gene-related peptide (CGRP)) levels in the spinal cord. It has been suggested previously that increased spinal CGRP may contribute to sustained morphine-mediated paradoxical pain sensitization and antinociceptive tolerance. Previous in vitro studies from our group indicated that Raf-1 kinase-mediated adenylyl cyclase superactivation played a crucial role in sustained morphine-mediated augmentation of basal and evoked CGRP release from cultured primary sensory neurons. The present study was aimed to evaluate the physiological significance of this molecular mechanism in vivo, in rats ...
DI-fusion, le Dépôt institutionnel numérique de lULB, est loutil de référencementde la production scientifique de lULB.Linterface de recherche DI-fusion permet de consulter les publications des chercheurs de lULB et les thèses qui y ont été défendues.
TY - JOUR. T1 - Coupling of a cloned rat dopamine-D2 receptor to inhibition of adenylyl cyclase and prolactin secretion. AU - Albert, Paul R.. AU - Neve, Kim. AU - Bunzow, James R.. AU - Civelli, Olivier. PY - 1990/2/5. Y1 - 1990/2/5. N2 - We have previously described a cDNA which encodes a binding site with the pharmacology of the D2-dopamine receptor (Bunzow, J. R., VanTol, H. H. M., Grandy, D. K., Albert, P., Salon, J., Christie, M., Machida, C., Neve, K. A., and Civelli, O. (1988) Nature 336, 783-787). We demonstrate here that this protein is a functional receptor, i.e. it couples to G-proteins to inhibit cAMP generation and hormone secretion. The cDNA was expressed in GH4C1 cells, a rat somatomammotrophic cell strain which lacks dopamine receptors. Stable transfectants were isolated and one clone, GH4ZR7, which had the highest levels of D2-dopamine receptor mRNA on ...
Within the compact cilia of the olfactory receptor neurons (ORNs) a cascade of enzymatic activity transduces the binding of an odorant molecule to a receptor into an electrical signal that can be transmitted to the brain. Odorant molecules bind to a receptor protein (R) coupled to an olfactory specific Gs-protein (G) and activate a type III adenylyl cyclase (AC), increasing intracellular cAMP levels. cAMP targets an olfactory-specific cyclic-nucleotide gated ion channel (CNG), allowing cations, particularly Na and Ca, to flow down their electrochemical gradients into the cell, depolarizing the ORN. Furthermore, the Ca entering the cell is able to activate a Ca-activated Cl channel, which would allow Cl to flow out of the cell, thus further increasing the depolarization. Elevated intracellular Ca causes adaptation by at least two different molecular steps: inhibition of the activity of ...
We have recently described the affinity chromatography purification of the turkey erythrocyte beta-adrenergic receptor. The minute amounts obtained initially precluded extensive biochemical characterization. To improve the yield of the receptor, the erythrocyte membranes have been prepared by a new method. This procedure resulted in a 10-fold higher receptor density in comparison with the membrane preparation used previously. The new membranes also contained a catecholamine-sensitive guanine triphosphatase and an adenylate cyclase sensitive to Gpp(NH)p and l-epinephrine. Solubilization by a double digitonin extraction resulted in a preparation containing 4-6 pmoles of 3H-dihydroalprenolol binding sites per mg of membrane protein. A single step of affinity chromatography on alprenolol-sepharose of the soluble digitonin extract resulted in an additional 1,000-fold purification of the receptor. ...
Previous pharmacological studies have indicated the possible existence of functional interactions between μ-, δ- and κ-opioid receptors in the CNS. We have investigated this issue using a genetic approach. Here we describe in vitro and in vivo functional activity of δ- and κ-opioid receptors in mice lacking the μ-opioid receptor (MOR). Measurements of agonist-induced [35S]GTPγS binding and adenylyl cyclase inhibition showed that functional coupling of δ- and κ-receptors to G-proteins is preserved in the brain of mutant mice. In the mouse vas deferens bioassay, deltorphin II and cyclic[d-penicillamine2,d-penicillamine5] enkephalin exhibited similar potency to inhibit smooth muscle contraction in both wild-type and MOR −/− mice. δ-Analgesia induced by deltorphin II was slightly diminished in mutant mice, when the tail flick test was used. Deltorphin II strongly reduced the respiratory frequency in wild-type ...
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We studied hearts from sham-operated and uninfected catheterized rabbits as well as from rabbits at early and late stages of cardiomyopathy and failure after 3 and 6 days of infection with Streptococcus viridans. No ultrastructural abnormalities or biochemical changes in membrane and myofibrillar activities were seen in 3-day uninfected hearts. In 6-day uninfected hearts there were decreased sarcolemmal M2+ ATPase, Na+-K+ ATPase, adenylate cyclase and calcium binding, microsomal calcium binding and uptake, and myofibrillar Ca2+-stimulated ATPase as well as increased mitochondrial calcium uptake. Slight ultrastructural changes also were apparent in 6-day uninfected hearts. At both early and late stages of infective cardiomyopathy and failure there were varying degrees of depression in sarcolemmal Mg2+ ATPase, Na+-K+ ATPase, adenylate cyclase and calcium binding, microsomal calcium binding, calcium uptake and basal ATPase, and myofibrillar ...
Hughes AR, Thastrup O, and Putney JW, Jr. Activation of calcium entry by the tumor promoter thapsigargin in parotid acinar cells. Evidence that an intracellular calcium pool and not an inositol phosphate regulate calcium fluxes at the plasma membrane. J Biol Chem 1989;264:12,266- 12,271. 45. Putney JW, Jr. Capacitative calcium entry revisited. Cell Calcium 1990;11:611-624. 46. Putney JW, Jr, Bird GSJ. The inositol phosphate-calcium signaling system in no-excitable cells. Endocr Rev 1993;14:610-631. Putney JW Jr. Type 3 inositol 1,4,5-trisphosphate receptor and capacitative calcium entry. Cell Calcium 1997;21:257-261. 13. Fagan KA, Graf RA, Tolman S, Schaack J, Cooper MF. Regulation of a Ca2+-sensitive adenylyl cyclase in an excitable cell. Role of voltage-gated versus capacitative Ca2+ entry. J Biol Chem 2000;275:40,187- 40,194. 14. Herms I, Schneider J, Dewachter I, Caluwaerts N, Kretzshmar H, Van Leuven F. Capacitative calcium entry is directly activated by mutant ...
Summary is not available for the mouse gene. This summary is for the human ortholog.] This gene encodes one of two cannabinoid receptors. The cannabinoids, principally delta-9-tetrahydrocannabinol and synthetic analogs, are psychoactive ingredients of marijuana. The cannabinoid receptors are members of the guanine-nucleotide-binding protein (G-protein) coupled receptor family, which inhibit adenylate cyclase activity in a dose-dependent, stereoselective and pertussis toxin-sensitive manner. The two receptors have been found to be involved in the cannabinoid-induced CNS effects (including alterations in mood and cognition) experienced by users of marijuana. Multiple transcript variants encoding two different protein isoforms have been described for this gene. [provided by RefSeq, May 2009 ...
Eviprostat is a popular phytotherapeutic agent for the treatment of lower urinary tract symptoms (LUTS). At present, the signaling mechanisms underlying its therapeutic effects are still poorly understood. Given that cAMP has been reported to suppress cell hyperplasia and hypertrophy in various pathological situations, we asked whether the effect of Eviprostat could be ascribed to the activation of the cAMP signaling pathway. In the study, exposure of cAMP response element (CRE)-secreted alkaline phosphatase (SEAP) (CRE-SEAP)-reporter cells to Eviprostat elevated SEAP secretion, which was associated with an increased phosphorylation of vasodilator-stimulated phosphoprotein (VASP) and cAMP-response element-binding protein (CREB), as well as enhanced expression of CRE-regulated protein connexin43, indicating an activation of the cAMP signaling pathway. Consistent with these observations, Eviprostat-induced expression of Cx43 was abolished in the presence of ...
The role of cyclic AMP in the octopaminergic modulation of the dorsal longitudinal flight muscles of the locust Schistocerca gregaria has been investigated. Several techniques have been used to elevate cyclic AMP levels in this tissue by mechanisms that bypass the receptor activation stage. These include the use of phosphodiesterase inhibitors to block the metabolism of cyclic nucleotides, the use of forskolin, the diterpene activator of adenylate cyclase, and the direct application of permeable and phosphodiesterase-resistant analogues of cyclic AMP. All these approaches can be shown to mimic the modulatory effects of octopamine on the flight muscle. Surprisingly, the phosphodiesterase inhibitors used were not able to potentiate the actions of octopamine on this preparation. Octopamine increases cyclic AMP levels in a similar fashion in all five motor units of this muscle, an effect that is selectively blocked by phentolamine, an α-adrenergic blocking agent ...
Guanylate cyclase activity of retinal rod outer segments was measured by an assay procedure that minimizes the technical problems caused by the high activity of cyclic nucleotide phosphodiesterase in neural tissue. Cyclase activity in rods is significantly higher than in brain. Moreover, activity is two-fold higher in dark-adapted rods than in light-bleached rods, a sensitivity that is lost when the preparation is treated with detergent. ...
In mammals, adenosine 3, 5-cyclic monophosphate (cAMP) is known to play highly important roles in sperm motility and acrosomal exocytosis. It is known to act through protein phosphorylation via PRKA and through the activation of guanine nucleotide exchange factors like EPAC. Sperm intracellular cAMP levels depend on the activity of adenylyl cyclases, mostly SACY, though transmembrane-containing adenylyl cyclases are also present, and on the activity of cyclic nucleotide phosphodiesterases (PDE) whose role is to degrade cAMP into 5-AMP. The PDE superfamily is subdivided into 11 families (PDE1 to 11), which act on either cAMP or cGMP, or on both cAMP and cGMP although with different enzymatic properties. PDE10, which is more effective on cAMP than cGMP, has been known for almost 15 years and is mostly studied in the brain where it is associated with neurological disorders. Although a high level of PDE10A gene expression is observed in the testis, information ...
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Purpose : Previous studies evaluating the impact of mutations in human retinal guanylyl cyclase (GUCY2D) known to be associated with Leber congenital amaurosis (LCA1) revealed wide heterogeneity in the biochemical properties of the affected cyclase - some of the mutations completely inactivated RetGC1 and some did not [1]. The purpose of this study was to test the mutant cyclase in vivo using AAV-mediated expression in mouse photoreceptors. Methods : The activities of LCA1-linked RetGC1 mutants and their abilities to bind GCAP and RD3 were assessed in vitro and in cyto, using cultured HEK293 cells expressing fluorescently labeled RetGC1, GCAP1 and RD3. AAV-mediated expression of human wild type, R1091x, and S248W RetGC1 [1] was evaluated in subretinally injected [2] RetGC1/RetGC2 double knockout (GCdKO) mice. ERG, immunofluorescence and biochemical properties of RetGC1s in the AAV-injected eyes were tested using the non-injected eyes as a ...
Human dopamine D3 receptor is a protein that is encoded by the dopamine receptor gene (DRD3).[2] The DRD3 gene codes for the D3 dopamine receptor that inhibits adenylyl cyclase through inhibitory G-proteins. G-protein coupled receptors are a family of transmembrane proteins that transmit chemical signals from outside the cell to cause changes inside of the cell. Adenylate cyclase is part of the G-protein receptors signaling and catalyze the conversion of ATP to cyclic AMP (cAMP).[3] The D3 receptor is located in the brain, suggesting that it plays a role in cognitive and emotional functions.[4] The human dopamine D3 receptor is membrane-bound and scattered in the cytoplasm. Receptor stimulation causes internalization of the ...
Multianalyte microphysiometry, a real-time instrument for simultaneous measurement of metabolic analytes in a microfluidic environment, was used to explore the effects of cholera toxin (CTx). Upon exposure of CTx to PC-12 cells, anaerobic respiration was triggered, measured as increases in acid and lactate production and a decrease in the oxygen uptake. We believe the responses observed are due to a CTx-induced activation of adenylate cyclase, increasing cAMP production and resulting in a switch to anaerobic respiration. Inhibitors (H-89, brefeldin A) and stimulators (forskolin) of cAMP were employed to modulate the CTx-induced cAMP responses. The results of this study show the utility of multianalyte microphysiometry to quantitatively determine the dynamic metabolic effects of toxins and affected pathways.
1. Platelet behaviour in vitro in relation to cyclic AMP was studied longitudinally during pregnancy and in the same women when they were not pregnant. Subjects comprised a group of healthy primigravidae and a group of women deemed at risk of pre-eclampsia, on the basis of a previous history of the condition.. 2. There was a progressive decline during pregnancy in sensitivity of platelets to inhibition of the arachidonic acid-induced release reaction by agents which act via cyclic AMP. This effect was maximum at 36 weeks gestation.. 3. Basal platelet cyclic AMP levels, and those in the presence of a phosphodiesterase inhibitor, did not change throughout the period of the study.. 4. By contrast, platelet cyclic AMP accumulation in response to a variety of adenylate cyclase stimulators was reduced from early pregnancy, throughout the gestational period, compared with post-natally. This effect was noted when platelets were incubated with prostaglandins acting via different ...
The decarboxylation of dopachrome to 5,6-dihydroxyindole (DHI) appears to be a major control point in the biosynthesis of melanin, in particular the conversion of dopachrome to 5,6-dihydroxyindole-2-carboxylic acid (DHICA). The recent discovery of a factor, DHICA stablin, that stabilizes DHICA and inhibits its conversion to DHI has added insight into the regulation of this intermediary compound. This study has shown that DHICA stablin activity is present in the melanosomal fraction of Cloudman murine melanoma cells and that this activity was observed by a new method using two complementary decarboxylase assays. When three known decarboxylase stabilizing cofactors (biotin, pyridoxal phosphate, and pyruvate) were added to melanosomal extracts, DHICA decarboxylase activity was enhanced but these factors did not decrease the lability of the decarboxylase enzyme. Protein kinases have been shown to mediate an adenylate cyclase system that is ...
The Expression of Vasoactive Intestinal Peptide Receptor 1 Is Negatively Modulated by MicroRNA 525-5p. . Biblioteca virtual para leer y descargar libros, documentos, trabajos y tesis universitarias en PDF. Material universiario, documentación y tareas realizadas por universitarios en nuestra biblioteca. Para descargar gratis y para leer online.
According to the Health Reviewers on forskolin free trial, this product is based entirely on natural ingredients. This makes it extremely safe. Its primary ingredient is extracted from herbal roots of an Indian plant known as Coleus Forskohlii. This primary ingredient facilitates the function of a particular enzyme known as cyclic adenosine monophosphate found in the walls of the cells. Also, known as adenylate cyclase, this enzyme increase of its level is tightly connected to the rise of insulin in the body.. Benefits of Forskolin supplements. Weight loss - The Forskolin supplements reviews show that this weight loss dietary supplement can produce weight loss by increasing the levels of cyclic adenosine monophosphate.. Proper body figure - The activity of the thyroid gland is affected by this supplement, too. The smooth muscles of the body begin to relax while the myocardium contracts more firmly. Out of all the blood cells that are used in the blood coagulation process, ...
Hudson, T H. and Johnson, G L., "Peptide mapping of adenylate cyclase regulatory proteins that are cholera toxin substrates." (1980). Subject Strain Bibliography 1980. 3108 ...
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Adenylate Cyclase: An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC 4.6.1.1.
Forskolin extract is really a supplement often known as a labdane diterpene.. It is a type of compound which is a lot like retinol, retinal, phytol, and is known to be both anti-microbial and anti-inflammatory.. It really is created by the benefits of forskolin that has played a huge role in Indian traditional medicine for centuries.. The plant itself is a member of the mint family and grows from the subtropical aspects of India, Burma, and Thailand.. Forskolin has proven to activate something called adenylate cyclase, which can be an enzyme working in the regulating a variety of cellular functions. This enzyme comes from ATP and utilized for signal transduction in a number of organisms.. Forskolin extract supplements cause an increase in cAMP levels which can promote weight reduction and increase memory formation and retention, especially when utilized in a CILTEP Stack with Artichoke Extract.. The principle means of action with this supplement is actually by the activation ...
It is widely accepted that cAMP regulates gene transcription principally by activating the protein kinase A (PKA)-targeted transcription factors. Here, we show that cAMP enhances the generation of 5-hydroxymethylcytosine (5hmC) in multiple cell types. 5hmC is converted from 5-methylcytosine (5mC) by Tet methylcytosine dioxygenases, for which Fe(II) is an essential cofactor. The promotion of 5hmC was mediated by a prompt increase of the intracellular labile Fe(II) pool (LIP). cAMP enhanced the acidification of endosomes for Fe(II) release to the LIP likely through RapGEF2. The effect of cAMP on Fe(II) and 5hmC was confirmed by adenylate cyclase activators, phosphodiesterase inhibitors, and most notably by stimulation of G protein-coupled receptors (GPCR). The transcriptomic changes caused by cAMP occurred in concert with 5hmC elevation in differentially transcribed genes. Collectively, these data show a ...
The effect of endogenous RGS proteins on receptor-mediated signaling has been studied in various systems by expressing RGS-insensitive or -sensitive Gαo (Jeong and Ikeda, 2000; Boutet-Robinet et al., 2003; Clark et al., 2003). Insensitivity of Gαo to endogenous RGS proteins increases receptor signaling to some, but not all, pathways that have been studied. In this work we have expressed RGS-insensitive and -sensitive Gαo in C6 glioma cells expressing the rat μ-opioid receptor. This allowed us to test two hypotheses, namely, that coupling of the μ-opioid receptor to Gαo can provide for adenylyl supersensitization and that RGS proteins decrease the degree of supersensitization because of their effect in shortening the lifetime of the active signaling molecule Gαo-GTP and its Gβγ counterpart. The results show the presence of active Gαo alone allows for the development of μ-opioid ...
Direct interactions between Ca2+ and cAMP have provided the basis for models predicting their interdependent oscillations in excitable cells (Cooper et al., 1995; Gorbunova and Spitzer, 2002; Rapp and Berridge, 1977; Yu et al., 2004). Central to all of these models are the actions of Ca2+ on Ca2+-inhibited and Ca2+-stimulated ACs respectively. Other key features include the feedback of cAMP onto Ca2+ channels and Ca2+/calmodulin-dependent PDE activity. Evidence of a dynamic interplay between Ca2+ and cAMP as a consequence of Ca2+-dependent PDE activity (PDE1C) was presented in a recent paper by Landa and colleagues (Landa et al., 2005). In this report, we reveal that cAMP oscillations can arise in non-excitable cells lacking both VGCCs and Ca2+-stimulated PDE activity. Artificially imposed or CCh-induced Ca2+ oscillations were shown to generate simple oscillations in cAMP matching the Ca2+ oscillation frequency. These oscillations were due to the stimulation of a Ca2+-sensitive AC (AC8), and ...
Schematic illustration of major second messenger pathways in the brain. Gs and Gi/o, respectively, mediate the ability of neurotransmitter receptors (R) to activate or inhibit adenylyl cyclase, the enzyme that catalyzes the synthesis of cAMP. Also shown in the figure is the ability of G-protein bg subunits, released potentially by any type of G-protein, or Ca2+/calmodulin to stimulate or inhibit different forms of adenylyl cyclase. Gq and perhaps Gi/o mediate the ability of neurotransmitter receptors to regulate phospholipase C (PLC), which metabolizes phosphatidylinositol (PI) into the second messengers inositol triphosphate (IP3) and diacylglycerol (DAG). IP3 then acts on specific IP3 receptors (IP3R) to increase intracellular levels of free Ca2+ (also a second messenger in brain) by releasing Ca2+ from internal stores. Increased levels of intracellular Ca2+ also result from the flux of ...
Research reagents for adenylate cyclase 1. Find antibodies, kits, proteins, RNAi and other reagents all backed by our Guarantee+.
The series of molecular signals generated as a consequence of a G-protein coupled receptor binding to its physiological ligand, where the pathway proceeds through inhibition of adenylyl cyclase activity and a subsequent decrease in the concentration of cy…
Adenylate cyclase type 5 (EC 4.6.1.1) (ATP pyrophosphate-lyase 5) (Adenylate cyclase type V) (Adenylyl cyclase 5) (Ca(2+)-inhibitable adenylyl cyclase ...
Visualization for given category : Effector, level : Node and node : ____Cyclases____Adenylate cyclases____Adenylate cyclase 5____Adenylate cyclase 5-Homo sapiens ...

Pituitary adenylate cyclase-activating polypeptide 38-mediated rin activation requires src and contributes to the regulation of...Pituitary adenylate cyclase-activating polypeptide 38-mediated rin activation requires src and contributes to the regulation of...

Article Pituitary adenylate cyclase-activating polypeptide 38-mediated rin activation requires src and contributes to the ... is a potent neuropeptide that acts through G-protein-coupled receptors. While it is well established that PACAP mediates both ... Instead, Rin loss attenuates PACAP38-mediated HSP27 activation by disrupting a cAMP-protein kinase A cascade. RNA interference- ... Pituitary adenylate cyclase-activating polypeptide 38-mediated .... Pituitary adenylate cyclase-activating polypeptide 38- ...
more infohttps://www.environmental-expert.com/articles/pituitary-adenylate-cyclase-activating-polypeptide-38-mediated-rin-activation-requires-src-and-contr-36524

WikiGenes - VIPR1 - vasoactive intestinal peptide receptor 1WikiGenes - VIPR1 - vasoactive intestinal peptide receptor 1

Peptide Agonist Docking in the N-terminal Ectodomain of a Class II G Protein-coupled Receptor, the VPAC1 Receptor: ... Pituitary adenylate cyclase-activating polypeptide and its receptors: from structure to functions. Vaudry, D., Gonzalez, B.J., ... Signal transduction through the vasoactive intestinal peptide receptor stimulates phosphorylation of the tyrosine kinase pp60c- ... Crucial role of two charged amino acids strictly conserved in class II G protein-coupled receptors. Couvineau, A., Lacapere, J. ...
more infohttps://www.wikigenes.org/e/gene/e/7433.html

The G Protein-Coupled Receptor Gpr1 Is a Nutrient Sensor That Regulates Pseudohyphal Differentiation in Saccharomyces...The G Protein-Coupled Receptor Gpr1 Is a Nutrient Sensor That Regulates Pseudohyphal Differentiation in Saccharomyces...

... of fbp1 transcription in Schizosaccharomyces pombe is partially regulated by adenylate cyclase activation by a G protein α ... 1992 Constitutive mutants of the protein kinase STE11 activate the pheromone response pathway in the absence of the G protein. ... The Gpr1 G protein-coupled receptor regulates filamentous growth: Our studies reveal that the G protein-coupled receptor Gpr1 ... The G protein-coupled receptor Gpr1 regulates filamentous growth: The G protein-coupled receptor homolog Gpr1 was identified in ...
more infohttp://www.genetics.org/content/154/2/609

adenocarcinoma of pituitary gland 2005:2010[pubdate] *count=100 - BioMedLib™ search engineadenocarcinoma of pituitary gland 2005:2010[pubdate] *count=100 - BioMedLib™ search engine

Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide. Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide, ... Vascular Endothelial Growth Factor Receptor-2; EC 2.7.11.24 / Mitogen-Activated Protein Kinases ... We show that proliferation and differentiation are intimately coupled in Rb(+/-) pituitary cells before tumor initiation. ... Receptors, Cell Surface; 0 / Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide; 0 / Receptors, Pituitary Adenylate ...
more infohttp://www.bmlsearch.com/?kwr=adenocarcinoma+of+pituitary+gland+2005:2010%5Bpubdate%5D&cxts=100&stmp=b0

Regulation of Dopamine D1 Receptor Function by Physical Interaction with the NMDA Receptors | Journal of NeuroscienceRegulation of Dopamine D1 Receptor Function by Physical Interaction with the NMDA Receptors | Journal of Neuroscience

D1 and D5 receptors preferentially couple to Gs proteins, stimulating the activity of adenylate cyclase and protein kinase A- ... Endocytosis of G-protein-coupled receptors: roles of G-protein-coupled receptor kinases and β-arrestin proteins. Prog Neurobiol ... Activation of NMDA receptor enhances D1 receptor membrane expression. Changes in G-protein-coupled receptor distribution by ... However, dopamine D5, but not D1, receptors exhibit functional cross-talk with GABAA receptors via a direct protein-protein ...
more infohttp://www.jneurosci.org/content/24/5/1149?ijkey=5d5af088766917c6997c24fbabcc5192c0ddf9fd&keytype2=tf_ipsecsha

Alamethicin - WikipediaAlamethicin - Wikipedia

... beta-adrenergic receptor-coupled adenylate cyclase, and cAMP-dependent protein kinase activities of cardiac sarcolemmal ... domain before being attached by a thioester bond to an Acyl Carrier Protein-like Peptidyl carrier protein. The growing chain is ... Explore structures of Alamethicin at the protein data bank Alamethicin in Norine From "A voltage-gated ion channel model ... Amino acids are initially adenylated by an "adenylylation" (A) ...
more infohttps://en.wikipedia.org/wiki/Alamethicin

Adenylate Cyclase/cAMP/Protein Kinase A Signaling Pathway Inhibits Endothelin Type A Receptor-Operated Ca2+ Entry Mediated via...Adenylate Cyclase/cAMP/Protein Kinase A Signaling Pathway Inhibits Endothelin Type A Receptor-Operated Ca2+ Entry Mediated via...

green fluorescent protein. GqPCR. Gq protein-coupled receptor. HA. hemagglutinin. HEK293. human embryonic kidney 293. HRP. ... protein kinase A. PKG. protein kinase G. ROCC. receptor-operated Ca2+ channel. ROCE. receptor-operated Ca2+ entry. Rp-8-Br-cAMP ... Adenylate Cyclase/cAMP/Protein Kinase A Signaling Pathway Inhibits Endothelin Type A Receptor-Operated Ca2+ Entry Mediated via ... Adenylate Cyclase/cAMP/Protein Kinase A Signaling Pathway Inhibits Endothelin Type A Receptor-Operated Ca2+ Entry Mediated via ...
more infohttp://jpet.aspetjournals.org/content/340/1/143

Pharmacology of Cannabinoid ReceptorsPharmacology of Cannabinoid Receptors

... both positively to mitogen-activated protein kinase (MAPK) and negatively to adenylate cyclase. ... these are CB1 and CB2 receptors, cloned in 1990 and 1993, respectively. Both of them are coupled through G-proteins, ... CB1 receptors from neurons and CB2 receptors from immune cells. Ligands for Cannabinoid Receptors. Endogenous agonists specific ... The discovery of cannabinoid receptors also instigated a quest for selective CB1 and CB2 receptor antagonists, with varying ...
more infohttps://www.news-medical.net/health/Pharmacology-of-Cannabinoid-Receptors.aspx

Bilayer lipid composition modulates the activity of dermaseptins, polycationic antimicrobial peptides | SpringerLinkBilayer lipid composition modulates the activity of dermaseptins, polycationic antimicrobial peptides | SpringerLink

... beta-adrenergic receptor-coupled adenylate cyclase, and cAMP-dependent protein kinase activities of cardiac sarcolemmal ... Homblé F, Cabiaux V, Ruysschaert J-M (1998) Channel or channel-like activity associated with pore-forming proteins or peptides ... Panchal RG, Smart ML, Bowser DN, Williams DA, Petrou S (2002) Pore-forming proteins and their application in biotechnology. ... Wroblewski H, Burlot R, Johansson KE (1978) Solubilization of Spiroplasma citri cell membrane proteins with the anionic ...
more infohttps://link.springer.com/article/10.1007/s00249-006-0047-9

Whole transcriptome analysis of the silicon response of the diatom Thalassiosira pseudonana | BMC Genomics | Full TextWhole transcriptome analysis of the silicon response of the diatom Thalassiosira pseudonana | BMC Genomics | Full Text

Finally, genes co-varying in expression with the SITs enabled identification of a new class of diatom-specific proteins ... cycle analysis indicates that assignment of the cell cycle specific stage of particular cyclins and cyclin dependent kinases ... protein degradation, glycosylation and transport, which provides a larger-scale picture of the processes involved. During ... containing a unique domain, and a putative silicon efflux protein. Analysis of the T. pseudonana microarray data has provided a ...
more infohttps://bmcgenomics.biomedcentral.com/articles/10.1186/1471-2164-13-499

JCI -
ATP receptor regulation of adenylate cyclase and protein kinase C activity in cultured renal LLC-PK1 cells.JCI - ATP receptor regulation of adenylate cyclase and protein kinase C activity in cultured renal LLC-PK1 cells.

These findings suggest the presence of functional P2y purinoceptors coupled to two signal transduction pathways in cultured ... ATP receptor regulation of adenylate cyclase and protein kinase C activity in cultured renal LLC-PK1 cells.. R J Anderson, R ... neither of two protein kinase C inhibitors (staurosporine and H-7) prevents ATP gamma S inhibition of AVP-stimulated adenylate ... Exposure of intact LLC-PK cells to ATP gamma S results in a significant increase in protein kinase C activity. However, ...
more infohttps://www.jci.org/articles/view/115191

The thrombospondin receptor integrin-associated protein (CD47) functionally couples to heterotrimeric Gi. - Semantic ScholarThe thrombospondin receptor integrin-associated protein (CD47) functionally couples to heterotrimeric Gi. - Semantic Scholar

Here we report that CD47, its beta3 integrin partner, and Gi proteins form a stable, detergent-soluble complex that can be ... This functional coupling of CD47 to heterotrimeric G proteins provides a mechanistic explanation for the biological effects of ... is a thrombospondin receptor that forms a signaling complex with beta3 integrins resulting in enhanced alphavbeta3-dependent ... Stimulates α2β1-Dependent Chemotaxis via GI-Mediated Inhibition of Adenylate Cyclase and Extracellular-Regulated Kinases. *Xue- ...
more infohttps://www.semanticscholar.org/paper/The-thrombospondin-receptor-integrin-associated-to-Frazier-Gao/7d14246814b9dd7fcda20cf76f750dafe1a3153c

ADCY2 - Adenylate cyclase type 2 - Homo sapiens (Human) - ADCY2 gene & proteinADCY2 - Adenylate cyclase type 2 - Homo sapiens (Human) - ADCY2 gene & protein

Functions in signaling cascades downstream of the muscarinic acetylcholine receptors (By similarity). ... Catalyzes the formation of the signaling molecule cAMP in response to G-protein signaling (PubMed:15385642). Down-stream ... activation of protein kinase A activity Source: Reactome. *adenylate cyclase-activating G-protein coupled receptor signaling ... adenylate cyclase-inhibiting G-protein coupled receptor signaling pathway Source: Reactome. *adenylate cyclase-modulating G- ...
more infohttp://www.uniprot.org/uniprot/Q08462

cgs1 - cAMP-dependent protein kinase regulatory subunit - Schizosaccharomyces pombe (strain 972 / ATCC 24843) (Fission yeast) -...cgs1 - cAMP-dependent protein kinase regulatory subunit - Schizosaccharomyces pombe (strain 972 / ATCC 24843) (Fission yeast) -...

... negative regulation of adenylate cyclase-activating glucose-activated G-protein coupled receptor signaling pathway, negative ... regulation of cAMP-dependent protein kinase activity, negative regulation of meiotic cell cycle, positive regulation of protein ... cAMP-dependent protein kinase complex, cytoplasm, cytosol, nucleus, cAMP binding, cAMP-dependent protein kinase regulator ... negative regulation of adenylate cyclase-activating glucose-activated G-protein coupled receptor signaling pathway Source: ...
more infohttp://www.uniprot.org/uniprot/P36600

Plus itPlus it

E2 action via G protein-coupled receptors, ERBB2, as well as activation of adenylate-cyclase and protein kinase A/PKC (47 , 50 ... p44/42 mitogen-activated protein kinase; Mek, MAP/ERK kinase; PKC, protein kinase C; EST, expressed sequence tag; MTT, 3-(4,5- ... Estrogen action via the G protein-coupled receptor, GPR30: stimulation of adenylyl cyclase and cAMP-mediated attenuation of the ... Protein kinase Cμ selectively activates the mitogen-activated protein kinase (MAPK) p42 pathway. FEBS Lett, 492: 39-44, 2001. ...
more infohttp://cancerres.aacrjournals.org/content/63/21/7158

EP3 (prostaglandin E2 receptor 3) expression is a prognostic factor for progression-free and overall survival in sporadic...EP3 (prostaglandin E2 receptor 3) expression is a prognostic factor for progression-free and overall survival in sporadic...

EP2 and EP4 receptor are coupled to Gs-protein/protein kinase A/adenylate cyclase and induce intracellular elevation of cyclic ... PGE2 mediates its effects via four G-protein coupled receptors, the EP receptors 1-4 with different intracellular signaling ... Patient data regarding patient age, hormone receptor status (estrogen receptor [ER], progesterone receptor [PR]), HER2- ... In prostate cancer e.g., EP3 II, an EP3 isoform coupled to Gi protein, was the major isoform found and EP3-expression also ...
more infohttps://link.springer.com/article/10.1186/s12885-018-4286-9

Relationship between Secondary Metabolism and Fungal Development | Microbiology and Molecular Biology ReviewsRelationship between Secondary Metabolism and Fungal Development | Microbiology and Molecular Biology Reviews

It involves a heterotrimeric G-protein-coupled receptor, adenylate cyclase, cyclic AMP (cAMP) signaling molecules, and protein ... Some proteins acting downstream of PKA in the G-protein signaling pathway also interact with components of the MAP kinase ... One protein, RasA, is a homolog of the yeast Ras proteins. The levels of activated RasA protein in fungal cells regulate the ... WD Protein RegulationA. nidulans rcoA encodes a member of the WD protein family. These proteins contain WD repeats, conserved ...
more infohttps://mmbr.asm.org/content/66/3/447?ijkey=350dfcb6e3cf77b77c91007162bed77be58ce17d&keytype2=tf_ipsecsha

Impairment of Mossy Fiber Long-Term Potentiation and Associative Learning in Pituitary Adenylate Cyclase Activating Polypeptide...Impairment of Mossy Fiber Long-Term Potentiation and Associative Learning in Pituitary Adenylate Cyclase Activating Polypeptide...

The pituitary adenylate cyclase activating polypeptide (PACAP) type I receptor PAC1 is a G-protein-coupled receptor that can ... most importantly the adenylate cyclase-protein kinase A (PKA) signal transduction pathway (Christophe, 1993). PAC1 binds the ... The pituitary adenylate cyclase activating polypeptide (PACAP) type I receptor (PAC1) is a G-protein-coupled receptor binding ... 1996b) cDNA cloning of a mouse pituitary adenylate cyclase-activating polypeptide receptor. Biochim Biophys Acta 1281:129-133. ...
more infohttp://www.jneurosci.org/content/21/15/5520

The human Na+/H+ exchanger 1 is a membrane scaffold protein for extracellular signal-regulated kinase 2 | Springer for Research...The human Na+/H+ exchanger 1 is a membrane scaffold protein for extracellular signal-regulated kinase 2 | Springer for Research...

... is an S/T kinase with more than 200 known substrates, and with critical roles in regulation of cell growth and differentiation ... Multiple receptors coupled to adenylate cyclase regulate Na-H exchange independent of cAMP. J Biol Chem. 1990;265:8989-92. ... Numerous hormones and growth factors acting via receptor tyrosine kinases or GTP-binding protein-coupled receptors can elicit ... Extracellular signal-regulated kinase 2 (ERK2) is a member of the mitogen-activated protein kinase (MAPK) family of kinases ...
more infohttps://rd.springer.com/article/10.1186/s12915-016-0252-7

GRK6 G protein-coupled receptor kinase 6 [Homo sapiens (human)] - Gene - NCBIGRK6 G protein-coupled receptor kinase 6 [Homo sapiens (human)] - Gene - NCBI

... is to activate adenylate cyclase, which in turn produces cAMP, leading to the activation of cAMP-dependent protein kinases ( ... GRK6 G protein-coupled receptor kinase 6 [Homo sapiens] GRK6 G protein-coupled receptor kinase 6 [Homo sapiens]. Gene ID:2870 ... G protein)-coupled receptor kinase subfamily of the Ser/Thr protein kinase family. The protein phosphorylates the activated ... Title: c-Src, Insulin-Like Growth Factor I Receptor, G-Protein-Coupled Receptor Kinases and Focal Adhesion Kinase are Enriched ...
more infohttps://www.ncbi.nlm.nih.gov/gene?Db=gene&Cmd=ShowDetailView&TermToSearch=2870&ordinalpos=2&itool=EntrezSystem2.PEntrez.Gene.Gene_ResultsPanel.Gene_RVDocSum

Probes for Neurotransmitter Receptors-Section 16.2 | Thermo Fisher Scientific - CNProbes for Neurotransmitter Receptors-Section 16.2 | Thermo Fisher Scientific - CN

Molecular Probes offers fluorescently labeled and unlabeled ligands for various cellular receptors, ion channels and ion ... fluorescent receptor ligands can provide a sensitive means of identifying and localizing some of the most pivotal molecules in ... Because receptor-mediated signal transduction underlies much of what occurs in cellular biochemistry and physiology, ... Receptors coupled to pertussis toxin (PTX)-sensitive G-proteins that inhibit adenylate cyclase activity. RPLC = Receptors ...
more infohttps://www.thermofisher.com/cn/zh/home/references/molecular-probes-the-handbook/probes-for-endocytosis-receptors-and-ion-channels/probes-for-neurotransmitter-receptors.html

PřF:C8155 Cell signaling - Course InformationPřF:C8155 Cell signaling - Course Information

Adenylate cyclase cascade and the mechanism of activation of protein kinase A. Phosphoinositide cascade and activation of ... signal transduction pathways initiated by the interaction of extracellular ligands with the G-protein coupled receptors. ( ... and protein kinases. Amplification function of receptor-effector-second messenger-protein kinase cascade). 5. Heterotrimeric G- ... Receptor tyrosine kinases (RTKs) and MAP kinase cascade. (Mechanism of action of growth factors receptors. Src and other ...
more infohttps://is.muni.cz/predmet/sci/C8155?lang=en

Principles of Biochemistry/Glucose, Glycogen and Diabetes - Wikibooks, open books for an open worldPrinciples of Biochemistry/Glucose, Glycogen and Diabetes - Wikibooks, open books for an open world

Glucagon activates adenylate cyclase through a seven transmembrane receptor coupled to Gs which, in turn, activates adenylate ... cAMP binds to and releases an active form of protein kinase A (PKA). Next, PKA phosphorylates phosphorylase kinase, which, in ... In the liver, epinephrine activates another G-protein-linked receptor that triggers a different cascade, resulting in the ... C-peptide should not be confused with c-reactive protein or Protein C.Newly diagnosed diabetes patients often get their C- ...
more infohttps://en.wikibooks.org/wiki/Principles_of_Biochemistry/Glucose,_Glycogen_and_Diabetes

Probes for Neurotransmitter Receptors-Section 16.2 | Thermo Fisher Scientific - JPProbes for Neurotransmitter Receptors-Section 16.2 | Thermo Fisher Scientific - JP

Molecular Probes offers fluorescently labeled and unlabeled ligands for various cellular receptors, ion channels and ion ... fluorescent receptor ligands can provide a sensitive means of identifying and localizing some of the most pivotal molecules in ... Because receptor-mediated signal transduction underlies much of what occurs in cellular biochemistry and physiology, ... Receptors coupled to pertussis toxin (PTX)-sensitive G-proteins that inhibit adenylate cyclase activity. RPLC = Receptors ...
more infohttps://www.thermofisher.com/jp/en/home/references/molecular-probes-the-handbook/probes-for-endocytosis-receptors-and-ion-channels/probes-for-neurotransmitter-receptors.html

Bupivacaine Inhibits Activation of Neuronal Spinal Extracellular Receptor-activated Kinase through Selective Effects on...Bupivacaine Inhibits Activation of Neuronal Spinal Extracellular Receptor-activated Kinase through Selective Effects on...

AC = adenylate cyclase; BK2R = bradykinin 2 receptor; cAMP = cyclic adenosine monophosphate; MEK = MAP kinase kinase; PLC = ... receptors and to metabotropic receptors mGluR; SP binds to G protein-coupled neurokinin 1 (NK-1) receptor. The activation of ... AC = adenylate cyclase; BK2R = bradykinin 2 receptor; cAMP = cyclic adenosine monophosphate; MEK = MAP kinase kinase; PLC = ... AC = adenylate cyclase; BK2R = bradykinin 2 receptor; cAMP = cyclic adenosine monophosphate; MEK = MAP kinase kinase; PLC = ...
more infohttp://anesthesiology.pubs.asahq.org/article.aspx?articleid=1923305
  • Here we show that the Ras-related Rin GTP-binding protein, a GTPase that is expressed predominantly in neurons, is regulated by PACAP38 signaling, and loss-of-function analysis demonstrates that Rin makes an essential contribution to PACAP38-mediated pheochromocytoma cell differentiation. (environmental-expert.com)
  • RNA interference-mediated HSP27 silencing suppresses both PACAP38- and Rin-mediated neurite outgrowth, while expression of a constitutively active Rin mutant increases both HSP27 protein and phospho-HSP27 levels, supporting a role for Rin-HSP27 signaling in neuronal differentiation. (environmental-expert.com)
  • R LG/ION = Receptors that promote ion fluxes directly because they are structurally linked to ion channels (members of the superfamily of ligand-gated ion channel receptors). (thermofisher.com)
  • Extracellular signal-regulated kinase 2 (ERK2) is an S/T kinase with more than 200 known substrates, and with critical roles in regulation of cell growth and differentiation and currently no membrane proteins have been linked to ERK2 scaffolding. (springer.com)
  • Receptor-operated Ca 2+ entry (ROCE) via transient receptor potential canonical channel 6 (TRPC6) is important machinery for an increase in intracellular Ca 2+ concentration triggered by the activation of G q protein-coupled receptors. (aspetjournals.org)
  • In contrast, the overall mechanism of spinal and epidural anesthesia may be more complex than simply the blockade of impulses in nerve roots, involving presynaptic and postsynaptic receptors as well as intracellular pathways. (asahq.org)
  • 12 Capsaicin, by binding to the ligand-gated vanilloid-sensitive transient receptor potential channel, TRPV1, on presynaptic terminals, directly catalyzes Ca +2 entry and also effects a depolarization that activates presynaptic calcium channels, as well as releasing Ca +2 from intracellular reticuli whose membranes contain TRPV1 channels, 13 all of which result in the release of glutamate and SP from primary nociceptor terminals. (asahq.org)
  • R PLC = Receptors promoting the hydrolysis of phosphatidylinositol 4,5-diphosphate (PIP 2 ) to inositol 1,4,5-triphosphate (IP 3 ), which increases intracellular Ca 2+ , and diacylglycerol (DAG), which activates protein kinase C (PKC). (thermofisher.com)
  • Binding of ATII to the AT1 receptor, a G protein-coupled receptor in the glomerulosa membrane, leads to the inhibition of potassium channels, depolarization and activation of voltage-gated calcium channels, and the release of calcium from intracellular stores (Figure 1 ). (frontiersin.org)
  • Our results demonstrate that the D1-NR1 physical interaction enables NMDA receptors to increase plasma membrane insertion of D1 receptors and provides a novel mechanism by which the activation of NMDA receptors upregulates D1 receptor function. (jneurosci.org)
  • Here, we identify the human Na + /H + exchanger 1 (hNHE1) as a membrane scaffold protein for ERK2 and show direct hNHE1-ERK1/2 interaction in cellular contexts. (springer.com)
  • However, although MAPKs are known to regulate the action of several membrane proteins and receptors, none of these scaffold proteins are themselves membrane proteins, requiring additional mechanisms for colocalization of the scaffold protein, the membrane protein, as well as the kinases. (springer.com)
  • 1 Local anesthetics may interact with many membrane phospholipids and proteins and thereby affect a variety of cellular activities. (asahq.org)
  • The existence of functional membrane-bound melatonin receptors on fish phagocytes was pharmacologically demonstrated. (healthdocbox.com)
  • It is an integral membrane protein and stimulates gastric acid secretion. (wikipedia.org)
  • Daly JW, Caceres J, Moni RW, Gusovsky F, Moos M Jr, Seamon KB, Milton K, Myers CW (1992) Frog secretions and hunting magic in the upper Amazon: identification of a peptide that interacts with an adenosine receptor. (springer.com)
  • For example, local anesthetics can affect several subtypes of protein kinase C (PKC), 2,3 adenosine 3′,5′-cyclic monophosphate-dependent kinase (PKA), 4 guanosine triphosphate-binding proteins (G proteins), 5 and many of the various receptors that activate them. (asahq.org)
  • In this study, we report that type II protein kinase A (PKA) is highly enriched in growth cone filopodia, and this spatial localization enables the coupling of cAMP signaling to its specific effectors to regulate guidance responses. (rupress.org)
  • Exposure to muscarinic agonists can also increase vagal efficacy by reducing β-adrenergic receptor responses. (aspetjournals.org)
  • Functional interactions between dopamine D1-like receptors and NMDA subtype glutamate receptors have been implicated in the maintenance of normal brain activity and neurological dysfunction. (jneurosci.org)
  • Here we report that NMDA receptors regulate D1 receptor function via a direct protein-protein interaction mediated by the carboxyl tail regions of both receptors. (jneurosci.org)
  • Furthermore, overexpression of mini-genes encoding either NR1 or D1 carboxyl tail fragments disrupts the D1-NR1 direct protein-protein interaction and abolishes NMDA-induced changes in both D1 cell surface expression and D1-mediated cAMP accumulation. (jneurosci.org)
  • Therefore, it is the subject of our present study to investigate whether the activation of NMDA receptors is able to regulate dopamine D1 receptor-mediated functions and the potential molecular mechanism underlying this process. (jneurosci.org)
  • NMDA receptors, activated by the principal excitatory neurotransmitter glutamate, are important in activity-dependent synaptic plasticity and excitotoxicity that underlie learning, memory, neural development, and many neurological disorders ( Michaelis, 1998 ). (jneurosci.org)
  • NMDA receptors, which mediate cation flux, exist as heteromeric assemblies of multiple subunits including NR1 and NR2 subunits ( Michaelis, 1998 ). (jneurosci.org)
  • Previous studies have shown the functional interaction between D1-like receptors and NMDA receptors. (jneurosci.org)
  • Nevertheless, this changed in the late 1980s when specific cannabinoid receptors were discovered. (news-medical.net)
  • Endogenous agonists specific for cannabinoid receptors are all eicosanoids. (news-medical.net)
  • Anandamide behaves as a partial agonist of cannabinoid receptors with slightly greater CB1 than CB2 affinity, but with much lower CB2 than CB1 efficacy . (news-medical.net)
  • The cannabinoid receptor agonists that have been used extensively in pharmacological experiments show equal binding affinity for both CB1 and CB2 receptors, or show merely marginal CB1 or CB2 selectivity. (news-medical.net)
  • The discovery of cannabinoid receptors also instigated a quest for selective CB1 and CB2 receptor antagonists, with varying degrees of success so far. (news-medical.net)
  • A critical advance in this regard was the establishment of a G-protein-mediated growth pathway in Aspergillus nidulans that regulates both asexual sporulation and natural product biosynthesis ( 55 ). (asm.org)
  • This process occurs in response to modifications of the cellular environment, including hormonal variations, and regulates the expression of subsets of proteins whose levels need to be rapidly adjusted. (frontiersin.org)
  • Among these endocannabinoids, arachidonoyl-ethanolamide (also known as anandamide) was among the first to be discovered, and there is compelling evidence that this ligand (as well as some of its metabolites) may also activate vanilloid VRI receptors. (news-medical.net)
  • The two p42 and p44 kDa MAP kinases are activated in a time- and dose-dependent manner. (biochemj.org)
  • However, the functional aspects of EP3 receptor in breast cancer and the way how EP3 may oppose the pro-tumorigenic effects of PGE2 elevation and COX-2 overexpression are not fully understood so far. (springer.com)
  • Contrary to expectations, morphine increased muscarinic receptor density in the right atrium and left ventricle by 17 and 34%, respectively, with no change in the apparent affinity of the receptor ( K D ). Morphine also increased the expression of the G protein G i α by 115 and 233%, respectively, in right atrial and left ventricular sarcolemmal membranes. (aspetjournals.org)
  • CB1 receptors are widely found in the central nervous system, but are also found in some peripheral tissues such as the heart, lungs, reproductive organs, gastrointestinal tissues, pituitary gland, sympathetic ganglia, urinary bladder and adrenal glands. (news-medical.net)
  • Significant correlations were identified between several clusters of drug-responsive genes and genes that discriminate estrogen receptor status or disease outcome in patient samples. (aacrjournals.org)
  • The majority of estrogen receptor status discriminators were not responsive in our dataset and are therefore likely to reflect underlying differences in histogenesis and disease progression rather than growth factor signaling. (aacrjournals.org)
  • For example, breast cancers that are ER 2 -positive often respond to 4-OHT and fulvestrant (ICI) that antagonize estrogen receptor signaling. (aacrjournals.org)