A family of structurally related proteins that are constitutively expressed and that negatively regulate cytokine-mediated SIGNAL TRANSDUCTION PATHWAYS. PIAS proteins inhibit the activity of signal transducers and activators of transcription.
An enzyme of the oxidoreductase class primarily found in PLANTS. It catalyzes reactions between linoleate and other fatty acids and oxygen to form hydroperoxy-fatty acid derivatives.
An enzyme that catalyzes the oxidation of arachidonic acid to yield 5-hydroperoxyarachidonate (5-HPETE) which is rapidly converted by a peroxidase to 5-hydroxy-6,8,11,14-eicosatetraenoate (5-HETE). The 5-hydroperoxides are preferentially formed in leukocytes.
An enzyme that catalyzes the oxidation of arachidonic acid to yield 12-hydroperoxyarachidonate (12-HPETE) which is itself rapidly converted by a peroxidase to 12-hydroxy-5,8,10,14-eicosatetraenoate (12-HETE). The 12-hydroperoxides are preferentially formed in PLATELETS.
Compounds that bind to and inhibit that enzymatic activity of LIPOXYGENASES. Included under this category are inhibitors that are specific for lipoxygenase subtypes and act to reduce the production of LEUKOTRIENES.
An enzyme that catalyzes the oxidation of arachidonic acid to yield 15-hydroperoxyarachidonate (15-HPETE) which is rapidly converted to 15-hydroxy-5,8,11,13-eicosatetraenoate (15-HETE). The 15-hydroperoxides are preferentially formed in NEUTROPHILS and LYMPHOCYTES.
Enzymes catalyzing the oxidation of arachidonic acid to hydroperoxyarachidonates. These products are then rapidly converted by a peroxidase to hydroxyeicosatetraenoic acids. The positional specificity of the enzyme reaction varies from tissue to tissue. The final lipoxygenase pathway leads to the leukotrienes. EC 1.13.11.- .
Compounds that bind to and inhibit the action of 5-LIPOXYGENASE-ACTIVATING PROTEINS.
A lipoxygenase metabolite of ARACHIDONIC ACID. It is a highly selective ligand used to label mu-opioid receptors in both membranes and tissue sections. The 12-S-HETE analog has been reported to augment tumor cell metastatic potential through activation of protein kinase C. (J Pharmacol Exp Ther 1995; 274(3):1545-51; J Natl Cancer Inst 1994; 86(15):1145-51)
Scaffolding proteins that play an important role in the localization and activation of 5-LIPOXYGENASE.
A family of biologically active compounds derived from arachidonic acid by oxidative metabolism through the 5-lipoxygenase pathway. They participate in host defense reactions and pathophysiological conditions such as immediate hypersensitivity and inflammation. They have potent actions on many essential organs and systems, including the cardiovascular, pulmonary, and central nervous system as well as the gastrointestinal tract and the immune system.
A potent lipoxygenase inhibitor that interferes with arachidonic acid metabolism. The compound also inhibits formyltetrahydrofolate synthetase, carboxylesterase, and cyclooxygenase to a lesser extent. It also serves as an antioxidant in fats and oils.
Eicosatetraenoic acids substituted in any position by one or more hydroxy groups. They are important intermediates in a series of biosynthetic processes leading from arachidonic acid to a number of biologically active compounds such as prostaglandins, thromboxanes, and leukotrienes.
The major metabolite in neutrophil polymorphonuclear leukocytes. It stimulates polymorphonuclear cell function (degranulation, formation of oxygen-centered free radicals, arachidonic acid release, and metabolism). (From Dictionary of Prostaglandins and Related Compounds, 1990)
An unsaturated, essential fatty acid. It is found in animal and human fat as well as in the liver, brain, and glandular organs, and is a constituent of animal phosphatides. It is formed by the synthesis from dietary linoleic acid and is a precursor in the biosynthesis of prostaglandins, thromboxanes, and leukotrienes.
A 1.5-kDa small ubiquitin-related modifier protein that can covalently bind via an isopeptide link to a number of cellular proteins. It may play a role in intracellular protein transport and a number of other cellular processes.
A dual inhibitor of both cyclooxygenase and lipoxygenase pathways. It exerts an anti-inflammatory effect by inhibiting the formation of prostaglandins and leukotrienes. The drug also enhances pulmonary hypoxic vasoconstriction and has a protective effect after myocardial ischemia.
A class of structurally related proteins of 12-20 kDa in size. They covalently modify specific proteins in a manner analogous to UBIQUITIN.
A type of POST-TRANSLATIONAL PROTEIN MODIFICATION by SMALL UBIQUITIN-RELATED MODIFIER PROTEINS (also known as SUMO proteins).
A plant genus of the family POACEAE. Finger millet or raggee (E. coracana) is an important food grain in southern Asia and parts of Africa.
A 20-carbon unsaturated fatty acid containing 4 alkyne bonds. It inhibits the enzymatic conversion of arachidonic acid to prostaglandins E(2) and F(2a).
(2S-(2 alpha,3 beta(1E,3E,5Z,8Z)))-3-(1,3,5,8-Tetradecatetraenyl)oxiranebutanoic acid. An unstable allylic epoxide, formed from the immediate precursor 5-HPETE via the stereospecific removal of a proton at C-10 and dehydration. Its biological actions are determined primarily by its metabolites, i.e., LEUKOTRIENE B4 and cysteinyl-leukotrienes. Alternatively, leukotriene A4 is converted into LEUKOTRIENE C4 by glutathione-S-transferase or into 5,6-di-HETE by the epoxide-hydrolase. (From Dictionary of Prostaglandins and Related Compounds, 1990)
Proteins that bind to and transfer CHOLESTEROL ESTERS between LIPOPROTEINS such as LOW-DENSITY LIPOPROTEINS and HIGH-DENSITY LIPOPROTEINS.
Eighteen-carbon essential fatty acids that contain two double bonds.
A class of compounds named after and generally derived from C20 fatty acids (EICOSANOIC ACIDS) that includes PROSTAGLANDINS; LEUKOTRIENES; THROMBOXANES, and HYDROXYEICOSATETRAENOIC ACIDS. They have hormone-like effects mediated by specialized receptors (RECEPTORS, EICOSANOID).
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.
A genus of beetles which infests grain products. Its larva is called mealworm.
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
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.
Transport proteins that carry specific substances in the blood or across cell membranes.
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.
The rate dynamics in chemical or physical systems.
Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed.
A homologous group of endogenous CYSTEINE PROTEINASE INHIBITORS. The cystatins inhibit most CYSTEINE ENDOPEPTIDASES such as PAPAIN, and other peptidases which have a sulfhydryl group at the active site.
A group of LEUKOTRIENES; (LTC4; LTD4; and LTE4) that is the major mediator of BRONCHOCONSTRICTION; HYPERSENSITIVITY; and other allergic reactions. Earlier studies described a "slow-reacting substance of ANAPHYLAXIS" released from lung by cobra venom or after anaphylactic shock. The relationship between SRS-A leukotrienes was established by UV which showed the presence of the conjugated triene. (From Merck Index, 11th ed)
A family of soil bacteria. It also includes some parasitic forms.
Peroxides produced in the presence of a free radical by the oxidation of unsaturated fatty acids in the cell in the presence of molecular oxygen. The formation of lipid peroxides results in the destruction of the original lipid leading to the loss of integrity of the membranes. They therefore cause a variety of toxic effects in vivo and their formation is considered a pathological process in biological systems. Their formation can be inhibited by antioxidants, such as vitamin E, structural separation or low oxygen tension.
A doubly unsaturated fatty acid, occurring widely in plant glycosides. It is an essential fatty acid in mammalian nutrition and is used in the biosynthesis of prostaglandins and cell membranes. (From Stedman, 26th ed)
A group of FLAVONOIDS characterized with a 4-ketone.
Compounds which inhibit or antagonize biosynthesis or actions of proteases (ENDOPEPTIDASES).
Screening techniques first developed in yeast to identify genes encoding interacting proteins. Variations are used to evaluate interplay between proteins and other molecules. Two-hybrid techniques refer to analysis for protein-protein interactions, one-hybrid for DNA-protein interactions, three-hybrid interactions for RNA-protein interactions or ligand-based interactions. Reverse n-hybrid techniques refer to analysis for mutations or other small molecules that dissociate known interactions.
Trihydroxy derivatives of eicosanoic acids. They are primarily derived from arachidonic acid, however eicosapentaenoic acid derivatives also exist. Many of them are naturally occurring mediators of immune regulation.
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.
An ionophorous, polyether antibiotic from Streptomyces chartreusensis. It binds and transports CALCIUM and other divalent cations across membranes and uncouples oxidative phosphorylation while inhibiting ATPase of rat liver mitochondria. The substance is used mostly as a biochemical tool to study the role of divalent cations in various biological systems.
A plant species of the genus SOLANUM, family SOLANACEAE. The starchy roots are used as food. SOLANINE is found in green parts.
Serine proteinase inhibitors which inhibit trypsin. They may be endogenous or exogenous compounds.
Compounds or agents that combine with cyclooxygenase (PROSTAGLANDIN-ENDOPEROXIDE SYNTHASES) and thereby prevent its substrate-enzyme combination with arachidonic acid and the formation of eicosanoids, prostaglandins, and thromboxanes.
Linear POLYPEPTIDES that are synthesized on RIBOSOMES and may be further modified, crosslinked, cleaved, or assembled into complex proteins with several subunits. The specific sequence of AMINO ACIDS determines the shape the polypeptide will take, during PROTEIN FOLDING, and the function of the protein.
A heterogeneous mixture of glycoproteins responsible for the gel structure of egg white. It has trypsin-inhibiting activity.
A non-steroidal anti-inflammatory agent (NSAID) that inhibits the enzyme cyclooxygenase necessary for the formation of prostaglandins and other autacoids. It also inhibits the motility of polymorphonuclear leukocytes.
A characteristic feature of enzyme activity in relation to the kind of substrate on which the enzyme or catalytic molecule reacts.
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.
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.
Established cell cultures that have the potential to propagate indefinitely.
An annual legume. The SEEDS of this plant are edible and used to produce a variety of SOY FOODS.
The parts of a macromolecule that directly participate in its specific combination with another molecule.
Exogenous or endogenous compounds which inhibit SERINE ENDOPEPTIDASES.
The relationship between the dose of an administered drug and the response of the organism to the drug.
Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures.
The species Oryctolagus cuniculus, in the family Leporidae, order LAGOMORPHA. Rabbits are born in burrows, furless, and with eyes and ears closed. In contrast with HARES, rabbits have 22 chromosome pairs.
A 6.6-kDa protein component of VERY-LOW-DENSITY LIPOPROTEINS; INTERMEDIATE-DENSITY LIPOPROTEINS; and HIGH-DENSITY LIPOPROTEINS. Apo C-I displaces APO E from lipoproteins, modulate their binding to receptors (RECEPTORS, LDL), and thereby decrease their clearance from plasma. Elevated Apo C-I levels are associated with HYPERLIPOPROTEINEMIA and ATHEROSCLEROSIS.
Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
Enzymes that catalyze the endohydrolysis of 1,4-alpha-glycosidic linkages in STARCH; GLYCOGEN; and related POLYSACCHARIDES and OLIGOSACCHARIDES containing 3 or more 1,4-alpha-linked D-glucose units.
Substances used to lower plasma CHOLESTEROL levels.
Derivatives of oxazolidin-2-one. They represent an important class of synthetic antibiotic agents.
A class of drugs designed to prevent leukotriene synthesis or activity by blocking binding at the receptor level.
Enzyme complexes that catalyze the formation of PROSTAGLANDINS from the appropriate unsaturated FATTY ACIDS, molecular OXYGEN, and a reduced acceptor.
A eukayrotic protein serine-threonine phosphatase subtype that dephosphorylates a wide variety of cellular proteins. The enzyme is comprised of a catalytic subunit and regulatory subunit. Several isoforms of the protein phosphatase catalytic subunit exist due to the presence of multiple genes and the alternative splicing of their mRNAs. A large number of proteins have been shown to act as regulatory subunits for this enzyme. Many of the regulatory subunits have additional cellular functions.
A CALCIUM-dependent, constitutively-expressed form of nitric oxide synthase found primarily in NERVE TISSUE.
The level of protein structure in which combinations of secondary protein structures (alpha helices, beta sheets, loop regions, and motifs) pack together to form folded shapes called domains. Disulfide bridges between cysteines in two different parts of the polypeptide chain along with other interactions between the chains play a role in the formation and stabilization of tertiary structure. Small proteins usually consist of only one domain but larger proteins may contain a number of domains connected by segments of polypeptide chain which lack regular secondary structure.
The degree of similarity between sequences of amino acids. This information is useful for the analyzing genetic relatedness of proteins and species.
A signal transducer and activator of transcription that mediates cellular responses to INTERFERONS. Stat1 interacts with P53 TUMOR SUPPRESSOR PROTEIN and regulates expression of GENES involved in growth control and APOPTOSIS.
Derivatives of propionic acid. Included under this heading are a broad variety of acid forms, salts, esters, and amides that contain the carboxyethane structure.
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.
A proteolytic enzyme obtained from Carica papaya. It is also the name used for a purified mixture of papain and CHYMOPAPAIN that is used as a topical enzymatic debriding agent. EC 3.4.22.2.
A family of cellular proteins that mediate the correct assembly or disassembly of polypeptides and their associated ligands. Although they take part in the assembly process, molecular chaperones are not components of the final structures.
Proteins prepared by recombinant DNA technology.
Exogenous and endogenous compounds which inhibit CYSTEINE ENDOPEPTIDASES.
An antineoplastic agent that inhibits DNA synthesis through the inhibition of ribonucleoside diphosphate reductase.
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.
The conjugation product of LEUKOTRIENE A4 and glutathione. It is the major arachidonic acid metabolite in macrophages and human mast cells as well as in antigen-sensitized lung tissue. It stimulates mucus secretion in the lung, and produces contractions of nonvascular and some VASCULAR SMOOTH MUSCLE. (From Dictionary of Prostaglandins and Related Compounds, 1990)
Proteins found in plants (flowers, herbs, shrubs, trees, etc.). The concept does not include proteins found in vegetables for which VEGETABLE PROTEINS is available.
Granular leukocytes having a nucleus with three to five lobes connected by slender threads of chromatin, and cytoplasm containing fine inconspicuous granules and stainable by neutral dyes.
The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.
Proteins and peptides that are involved in SIGNAL TRANSDUCTION within the cell. Included here are peptides and proteins that regulate the activity of TRANSCRIPTION FACTORS and cellular processes in response to signals from CELL SURFACE RECEPTORS. Intracellular signaling peptide and proteins may be part of an enzymatic signaling cascade or act through binding to and modifying the action of other signaling factors.
Phospholipases that hydrolyze one of the acyl groups of phosphoglycerides or glycerophosphatidates.
The biosynthesis of RNA carried out on a template of DNA. The biosynthesis of DNA from an RNA template is called REVERSE TRANSCRIPTION.
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.
Cell-surface receptors that bind LEUKOTRIENES with high affinity and trigger intracellular changes influencing the behavior of cells. The leukotriene receptor subtypes have been tentatively named according to their affinities for the endogenous leukotrienes LTB4; LTC4; LTD4; and LTE4.
Phospholipases that hydrolyze the acyl group attached to the 2-position of PHOSPHOGLYCERIDES.
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.
A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.
A class of phenolic acids related to chlorogenic acid, p-coumaric acid, vanillic acid, etc., which are found in plant tissues. It is involved in plant growth regulation.
A family of multisubunit cytoskeletal motor proteins that use the energy of ATP hydrolysis to power a variety of cellular functions. Dyneins fall into two major classes based upon structural and functional criteria.
A group of 1,2-benzenediols that contain the general formula R-C6H5O2.
Intracellular fluid from the cytoplasm after removal of ORGANELLES and other insoluble cytoplasmic components.
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.
7-carbon saturated monocarboxylic acids.
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.
Eighteen-carbon essential fatty acids that contain three double bonds.
Azoles of one NITROGEN and two double bonds that have aromatic chemical properties.
A group of enzymes removing the SERINE- or THREONINE-bound phosphate groups from a wide range of phosphoproteins, including a number of enzymes which have been phosphorylated under the action of a kinase. (Enzyme Nomenclature, 1992)
White blood cells. These include granular leukocytes (BASOPHILS; EOSINOPHILS; and NEUTROPHILS) as well as non-granular leukocytes (LYMPHOCYTES and MONOCYTES).
The introduction of a phosphoryl group into a compound through the formation of an ester bond between the compound and a phosphorus moiety.
A biologically active principle of SRS-A that is formed from LEUKOTRIENE D4 via a peptidase reaction that removes the glycine residue. The biological actions of LTE4 are similar to LTC4 and LTD4. (From Dictionary of Prostaglandins and Related Compounds, 1990)
Non-nucleated disk-shaped cells formed in the megakaryocyte and found in the blood of all mammals. They are mainly involved in blood coagulation.
A signal transducer and activator of transcription that mediates cellular responses to INTERLEUKIN-6 family members. STAT3 is constitutively activated in a variety of TUMORS and is a major downstream transducer for the CYTOKINE RECEPTOR GP130.
The characteristic 3-dimensional shape of a protein, including the secondary, supersecondary (motifs), tertiary (domains) and quaternary structure of the peptide chain. PROTEIN STRUCTURE, QUATERNARY describes the conformation assumed by multimeric proteins (aggregates of more than one polypeptide chain).
Within a eukaryotic cell, a membrane-limited body which contains chromosomes and one or more nucleoli (CELL NUCLEOLUS). The nuclear membrane consists of a double unit-type membrane which is perforated by a number of pores; the outermost membrane is continuous with the ENDOPLASMIC RETICULUM. A cell may contain more than one nucleus. (From Singleton & Sainsbury, Dictionary of Microbiology and Molecular Biology, 2d ed)
Compounds based on benzeneacetamide, that are similar in structure to ACETANILIDES.
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.
Elements of limited time intervals, contributing to particular results or situations.
FATTY ACIDS in which the carbon chain contains one or more double or triple carbon-carbon bonds.
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.
Immature ERYTHROCYTES. In humans, these are ERYTHROID CELLS that have just undergone extrusion of their CELL NUCLEUS. They still contain some organelles that gradually decrease in number as the cells mature. RIBOSOMES are last to disappear. Certain staining techniques cause components of the ribosomes to precipitate into characteristic "reticulum" (not the same as the ENDOPLASMIC RETICULUM), hence the name reticulocytes.
A cell line derived from cultured tumor cells.
An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH.
A 20-carbon-chain fatty acid, unsaturated at positions 8, 11, and 14. It differs from arachidonic acid, 5,8,11,14-eicosatetraenoic acid, only at position 5.
The facilitation of a chemical reaction by material (catalyst) that is not consumed by the reaction.
A family of enzymes that catalyze the conversion of ATP and a protein to ADP and a phosphoprotein.
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.
CELL LINES derived from the CV-1 cell line by transformation with a replication origin defective mutant of SV40 VIRUS, which codes for wild type large T antigen (ANTIGENS, POLYOMAVIRUS TRANSFORMING). They are used for transfection and cloning. (The CV-1 cell line was derived from the kidney of an adult male African green monkey (CERCOPITHECUS AETHIOPS).)
The molecular designing of drugs for specific purposes (such as DNA-binding, enzyme inhibition, anti-cancer efficacy, etc.) based on knowledge of molecular properties such as activity of functional groups, molecular geometry, and electronic structure, and also on information cataloged on analogous molecules. Drug design is generally computer-assisted molecular modeling and does not include pharmacokinetics, dosage analysis, or drug administration analysis.
The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.
Enzymes that catalyze reversibly the formation of an epoxide or arene oxide from a glycol or aromatic diol, respectively.
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.
Azoles of two nitrogens at the 1,2 positions, next to each other, in contrast with IMIDAZOLES in which they are at the 1,3 positions.
A group of compounds that contain the structure SO2NH2.
The sum of the weight of all the atoms in a molecule.
A serine endopeptidase secreted by the pancreas as its zymogen, CHYMOTRYPSINOGEN and carried in the pancreatic juice to the duodenum where it is activated by TRYPSIN. It selectively cleaves aromatic amino acids on the carboxyl side.
A microtubule-associated mechanical adenosine triphosphatase, that uses the energy of ATP hydrolysis to move organelles along microtubules toward the plus end of the microtubule. The protein is found in squid axoplasm, optic lobes, and in bovine brain. Bovine kinesin is a heterotetramer composed of two heavy (120 kDa) and two light (62 kDa) chains. EC 3.6.1.-.
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.
Processes that stimulate the GENETIC TRANSCRIPTION of a gene or set of genes.
Cells grown in vitro from neoplastic tissue. If they can be established as a TUMOR CELL LINE, they can be propagated in cell culture indefinitely.
A class of cell surface leukotriene receptors with a preference for leukotriene B4. Leukotriene B4 receptor activation influences chemotaxis, chemokinesis, adherence, enzyme release, oxidative bursts, and degranulation in polymorphonuclear leukocytes. There are at least two subtypes of these receptors. Some actions are mediated through the inositol phosphate and diacylglycerol second messenger systems.
A stable, physiologically active compound formed in vivo from the prostaglandin endoperoxides. It is important in the platelet-release reaction (release of ADP and serotonin).
Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.
ENDOPEPTIDASES which have a cysteine involved in the catalytic process. This group of enzymes is inactivated by CYSTEINE PROTEINASE INHIBITORS such as CYSTATINS and SULFHYDRYL REAGENTS.
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.
Eighteen-carbon cyclopentyl polyunsaturated fatty acids derived from ALPHA-LINOLENIC ACID via an oxidative pathway analogous to the EICOSANOIDS in animals. Biosynthesis is inhibited by SALICYLATES. A key member, jasmonic acid of PLANTS, plays a similar role to ARACHIDONIC ACID in animals.
A chemical reaction in which an electron is transferred from one molecule to another. The electron-donating molecule is the reducing agent or reductant; the electron-accepting molecule is the oxidizing agent or oxidant. Reducing and oxidizing agents function as conjugate reductant-oxidant pairs or redox pairs (Lehninger, Principles of Biochemistry, 1982, p471).
A creeping annual plant species of the CUCURBITACEAE family. It has a rough succulent, trailing stem and hairy leaves with three to five pointed lobes.
Electrophoresis in which a polyacrylamide gel is used as the diffusion medium.
Diffusible gene products that act on homologous or heterologous molecules of viral or cellular DNA to regulate the expression of 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.-.
One of the mechanisms by which CELL DEATH occurs (compare with NECROSIS and AUTOPHAGOCYTOSIS). Apoptosis is the mechanism responsible for the physiological deletion of cells and appears to be intrinsically programmed. It is characterized by distinctive morphologic changes in the nucleus and cytoplasm, chromatin cleavage at regularly spaced sites, and the endonucleolytic cleavage of genomic DNA; (DNA FRAGMENTATION); at internucleosomal sites. This mode of cell death serves as a balance to mitosis in regulating the size of animal tissues and in mediating pathologic processes associated with tumor growth.
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.
Dioxygenases that catalyze the peroxidation of methylene-interrupted UNSATURATED FATTY ACIDS.
A chemically diverse group of substances produced by various tissues in the body that cause slow contraction of smooth muscle; they have other intense but varied pharmacologic activities.
Any member of the group of ENDOPEPTIDASES containing at the active site a serine residue involved in catalysis.
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.
A diverse class of enzymes that interact with UBIQUITIN-CONJUGATING ENZYMES and ubiquitination-specific protein substrates. Each member of this enzyme group has its own distinct specificity for a substrate and ubiquitin-conjugating enzyme. Ubiquitin-protein ligases exist as both monomeric proteins multiprotein complexes.
An acridine derivative formerly widely used as an antimalarial but superseded by chloroquine in recent years. It has also been used as an anthelmintic and in the treatment of giardiasis and malignant effusions. It is used in cell biological experiments as an inhibitor of phospholipase A2.
The most common and most biologically active of the mammalian prostaglandins. It exhibits most biological activities characteristic of prostaglandins and has been used extensively as an oxytocic agent. The compound also displays a protective effect on the intestinal mucosa.
Proteins which bind to DNA. The family includes proteins which bind to both double- and single-stranded DNA and also includes specific DNA binding proteins in serum which can be used as markers for malignant diseases.
The normality of a solution with respect to HYDROGEN ions; H+. It is related to acidity measurements in most cases by pH = log 1/2[1/(H+)], where (H+) is the hydrogen ion concentration in gram equivalents per liter of solution. (McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)
DNA sequences which are recognized (directly or indirectly) and bound by a DNA-dependent RNA polymerase during the initiation of transcription. Highly conserved sequences within the promoter include the Pribnow box in bacteria and the TATA BOX in eukaryotes.
A group of compounds that contain a bivalent O-O group, i.e., the oxygen atoms are univalent. They can either be inorganic or organic in nature. Such compounds release atomic (nascent) oxygen readily. Thus they are strong oxidizing agents and fire hazards when in contact with combustible materials, especially under high-temperature conditions. The chief industrial uses of peroxides are as oxidizing agents, bleaching agents, and initiators of polymerization. (From Hawley's Condensed Chemical Dictionary, 11th ed)
Endogenous substances, usually proteins, which are effective in the initiation, stimulation, or termination of the genetic transcription process.
The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
Benzene rings which contain two ketone moieties in any position. They can be substituted in any position except at the ketone groups.
Agents that inhibit PROTEIN KINASES.
Small double-stranded, non-protein coding RNAs (21-31 nucleotides) involved in GENE SILENCING functions, especially RNA INTERFERENCE (RNAi). Endogenously, siRNAs are generated from dsRNAs (RNA, DOUBLE-STRANDED) by the same ribonuclease, Dicer, that generates miRNAs (MICRORNAS). The perfect match of the siRNAs' antisense strand to their target RNAs mediates RNAi by siRNA-guided RNA cleavage. siRNAs fall into different classes including trans-acting siRNA (tasiRNA), repeat-associated RNA (rasiRNA), small-scan RNA (scnRNA), and Piwi protein-interacting RNA (piRNA) and have different specific gene silencing functions.
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.
Presence of warmth or heat or a temperature notably higher than an accustomed norm.
A variation of the PCR technique in which cDNA is made from RNA via reverse transcription. The resultant cDNA is then amplified using standard PCR protocols.
An inducibly-expressed subtype of prostaglandin-endoperoxide synthase. It plays an important role in many cellular processes and INFLAMMATION. It is the target of COX2 INHIBITORS.
Chromatography on non-ionic gels without regard to the mechanism of solute discrimination.
A class of enzymes that catalyze the formation of a bond between two substrate molecules, coupled with the hydrolysis of a pyrophosphate bond in ATP or a similar energy donor. (Dorland, 28th ed) EC 6.
Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques.
One of the biologically active principles of SRS-A. It is generated from LEUKOTRIENE C4 after partial hydrolysis of the peptide chain, i.e., cleavage of the gamma-glutamyl portion. Its biological actions include stimulation of vascular and nonvascular smooth muscle, and increases in vascular permeability. (From Dictionary of Prostaglandins and Related Compounds, 1990)
Cell surface proteins that bind eicosanoids with high affinity and trigger intracellular changes influencing the behavior of cells. Among the eicosanoid receptors are receptors for the prostaglandins, thromboxanes, and leukotrienes.
A microanalytical technique combining mass spectrometry and gas chromatography for the qualitative as well as quantitative determinations of compounds.
A phospholipid derivative formed by PLATELETS; BASOPHILS; NEUTROPHILS; MONOCYTES; and MACROPHAGES. It is a potent platelet aggregating agent and inducer of systemic anaphylactic symptoms, including HYPOTENSION; THROMBOCYTOPENIA; NEUTROPENIA; and BRONCHOCONSTRICTION.
A group of alicyclic hydrocarbons with the general formula R-C5H9.
Enzymes of the isomerase class that catalyze the oxidation of one part of a molecule with a corresponding reduction of another part of the same molecule. They include enzymes converting aldoses to ketoses (ALDOSE-KETOSE ISOMERASES), enzymes shifting a carbon-carbon double bond (CARBON-CARBON DOUBLE BOND ISOMERASES), and enzymes transposing S-S bonds (SULFUR-SULFUR BOND ISOMERASES). (From Enzyme Nomenclature, 1992) EC 5.3.
A group of compounds derived from unsaturated 20-carbon fatty acids, primarily arachidonic acid, via the cyclooxygenase pathway. They are extremely potent mediators of a diverse group of physiological processes.
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.
Proteins, usually acting in oxidation-reduction reactions, containing iron but no porphyrin groups. (Lehninger, Principles of Biochemistry, 1993, pG-10)
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.
A large lobed glandular organ in the abdomen of vertebrates that is responsible for detoxification, metabolism, synthesis and storage of various substances.
The level of protein structure in which regular hydrogen-bond interactions within contiguous stretches of polypeptide chain give rise to alpha helices, beta strands (which align to form beta sheets) or other types of coils. This is the first folding level of protein conformation.
A positive regulatory effect on physiological processes at the molecular, cellular, or systemic level. At the molecular level, the major regulatory sites include membrane receptors, genes (GENE EXPRESSION REGULATION), mRNAs (RNA, MESSENGER), and proteins.
A serine endopeptidase that is formed from TRYPSINOGEN in the pancreas. It is converted into its active form by ENTEROPEPTIDASE in the small intestine. It catalyzes hydrolysis of the carboxyl group of either arginine or lysine. EC 3.4.21.4.
7-Hydroxycoumarins. Substances present in many plants, especially umbelliferae. Umbelliferones are used in sunscreen preparations and may be mutagenic. Their derivatives are used in liver therapy, as reagents, plant growth factors, sunscreens, insecticides, parasiticides, choleretics, spasmolytics, etc.
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.
Conjugated protein-carbohydrate compounds including mucins, mucoid, and amyloid glycoproteins.
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.
Structurally related forms of an enzyme. Each isoenzyme has the same mechanism and classification, but differs in its chemical, physical, or immunological characteristics.
Any of various enzymatically catalyzed post-translational modifications of PEPTIDES or PROTEINS in the cell of origin. These modifications include carboxylation; HYDROXYLATION; ACETYLATION; PHOSPHORYLATION; METHYLATION; GLYCOSYLATION; ubiquitination; oxidation; proteolysis; and crosslinking and result in changes in molecular weight and electrophoretic motility.
Proteins found in the nucleus of a cell. Do not confuse with NUCLEOPROTEINS which are proteins conjugated with nucleic acids, that are not necessarily present in the nucleus.
All of the processes involved in increasing CELL NUMBER including CELL DIVISION.
The study of crystal structure using X-RAY DIFFRACTION techniques. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
All-purpose surfactant, wetting agent, and solubilizer used in the drug, cosmetics, and food industries. It has also been used in laxatives and as cerumenolytics. It is usually administered as either the calcium, potassium, or sodium salt.
Anti-inflammatory agents that are non-steroidal in nature. In addition to anti-inflammatory actions, they have analgesic, antipyretic, and platelet-inhibitory actions.They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins. Inhibition of prostaglandin synthesis accounts for their analgesic, antipyretic, and platelet-inhibitory actions; other mechanisms may contribute to their anti-inflammatory effects.

Involvement of 5-lipoxygenase activating protein in the amyloidotic phenotype of an Alzheimer's disease mouse model. (1/4)

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Pharmacodynamics, pharmacokinetics and safety of GSK2190915, a novel oral anti-inflammatory 5-lipoxygenase-activating protein inhibitor. (2/4)

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An inhibitor of leukotriene synthesis affects vasopressin secretion following osmotic stimulus in rats. (3/4)

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FLAP pharmacological blockade modulates metabolism of endogenous tau in vivo . (4/4)

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FLAP antibody, Internal (arachidonate 5-lipoxygenase-activating protein) for IHC-P, WB. Anti-FLAP pAb (GTX89246) is tested in Human samples. 100% Ab-Assurance.
Intracerebral injection of brain extracts containing amyloid or tau aggregates in transgenic animals can induce cerebral amyloidosis and tau pathology. We extracted pure populations of tau oligomers directly from the cerebral cortex of Alzheimer disease (AD) brain. These oligomers are potent inhibit …
Serum-alone treatment of monocytes did not induce any detectable increase in IL-1β, TNF-α or IL-6 secretion. However, pre-treatment with PFAPA-IN serum did result in significantly more IL-1β secretion following LPSup stimulation as compared to PFAPA-OUT serum pretreatment (330.8 ± 181.5 and 173.5 ± 100.1 pg/ml respectively; n=9; p,0.05). There was no modulation in the levels of TNF-α and IL-6 under the present conditions, arguing for a process specific for the IL-1β pathway. ...
Diabetic patients exhibit a reduction in β cells, which secrete insulin to help regulate glucose homeostasis; however, little is known about the factors that regulate proliferation of these cells in human pancreas. Access to primary human β cells is limited and a challenge for both functional studies and drug discovery progress. We previously reported the generation of a human β cell line (EndoC-βH1) that was generated from human fetal pancreas by targeted oncogenesis followed by in vivo cell differentiation in mice. EndoC-βH1 cells display many functional properties of adult β cells, including expression of β cell markers and insulin secretion following glucose stimulation; however, unlike primary β cells, EndoC-βH1 cells continuously proliferate. Here, we devised a strategy to generate conditionally immortalized human β cell lines based on Cre-mediated excision of the immortalizing transgenes. The resulting cell line (EndoC-βH2) could be massively amplified in vitro. After ...
Tips to survive allergy season - Every spring trees and plants release pollen into the air to fertilize other plants. The released pollen can potentially enter an individuals nasal passages and trigger an immune response. This process affects mil...
To compare the roles of soluble CLP and membrane-bound FLAP in LT biosynthesis, we knocked down these proteins in the human monocytic cell line MM6. 5LO activity was determined in cells stimulated by four different protocols. Our results indicate that the presence of CLP in MM6 cells increased 5LO activity in all conditions (Figs. 1 and 2 and Table S1). Thus, CLP can support 5LO activity in intact cells as well, complementing previous in vitro data (12, 17). CLP is not absolutely crucial, however; some 5LO activity remained in all incubations of CLP knockdown cells. FLAP knockdown had only minor effects in incubations including exogenous AA, but 5LO product formation from endogenous substrate was greatly reduced. This finding is in accordance with the ideas that FLAP has a role in providing endogenous substrate to 5LO at the nuclear membrane (6) and that exogenous AA can be converted by 5LO in a FLAP-independent manner.. When cells are stimulated to produce LTs, 5LO typically translocates to the ...
Aggregation of the microtubule‐associated protein tau is a key feature of Alzheimers disease and other so‐called tauopathies, yet what causes this protein to aggregate and what renders it toxic is only slowly being revealed. Because tau spreads in a stereotypical pattern through the diseased brain, it has been proposed that it possesses prion‐like properties, with aggregation‐prone tau facilitating the conversion of naïve tau into toxic forms. The current study by Wegmann et al (2015) addresses whether tau fulfils classical prion criteria by assessing its spreading and toxicity in the absence of endogenous tau. Using different transgenic and viral paradigms, the authors demonstrate that, although tau still propagates in this scenario, there is a decrease in its misfolding and neurotoxicity. They therefore conclude that tau is not a genuine prion, at least when the current definition of these infectious proteins is applied.. See also: S Wegmann et al (December 2015) ...
The researchers first asked how aggregation influences pathology. In the case of the full-length proaggregation form of tau, the scientists saw a pathological conformation of tau (i.e., MC1 staining) and hyperphosphorylation at many sites in the hippocampus after 6 months, but no tangle formation. They saw only minor changes in phosphorylation with the antiaggregation mutant. All changes were reversible when tau expression was switched off for 6 weeks. In the case of the short form of tau, the proaggregation mutant began developing tangles in the entorhinal cortex at 3 months and progressed with age, even at low levels of exogenous tau (0.7 of endogenous), whereas the antiaggregation mutants showed no tangles. The proaggregation short form of tau nucleated aggregates, which then grew to incorporate both transgenic and endogenous tau. In old mice, the proaggregation, but not the antiaggregation mutants caused synaptic loss and neurodegeneration in the dentate gyrus of the hippocampus. In ...
The prediabetic state is characterized by normal glucose tolerance but decreased insulin secretion following glucose stimulation. In spite of our earlier beliefs, this state is not always devoid of metabolic consequences. Thus, the disappearance rate of intravenously administered glucose (k-value), although within the normal range, is significantly lower than in the control group. In a few prediabetics the regulation of hepatic glucose output resembles that of diabetics. In some, the lipolytic response to physical exercise is increased to the extent found in manifest diabetes. Furthermore, prediabetic mothers may give birth to children with diabetic fetopathy. Many of the newborns of these women show high k-values as do children of diabetic women.. The decreased insulin output of prediabetics and mild diabetics is probably due to a decreased sensitivity for glucose of a specific receptor of the beta cells of the pancreas. This suggestion is supported by the finding that both prediabetics and ...
Colostrum Colostrum is the first mammary secretion following the birth of a newborn, prior to lactation. Its properties are highly beneficial for health, growth, development and immune system functions. Bovine Colostrum is nearly identical to human Colostrum, and can benefit growth and immunity, muscle mass development, and bone and joint health in children and adults of all ages. Bovine Colostrum, is used for immune system enhancement, antibacterial, viral, and fungal protection, anti-inflammatory effects, wound healing, gastrointestinal problems, allergies, fatigue and muscle pain relief, to promote growth and muscle mass development and to promote bone and joint health. Collected from U.S. pasture-fed cows, FoodScience Colostrum is pesticide, antibiotic, and hormone free. Each enteric coated capsule contains: 600 mg Bovine Colostrum Ig (Immunoglobulins) 180 mg. Other ingredients: gelatin, water. As a dietary supplement, take 1 capsule on a empty stomach, one to three times daily. This statement has
"Inhibition of five lipoxygenase activating protein (FLAP) by MK-886 decreases atherosclerosis in apoE/LDLR-double knockout mice ... Zileuton is a specific inhibitor of 5-lipoxygenase and thus inhibits leukotriene (LTB4, LTC4, LTD4, and LTE4) formation. Both ... Another important activity for hyperforin is a dual inhibitor of cyclooxygenase-1 and 5-lipoxygenase [59]. Moreover, this ... is a medication which functions as a leukotriene-related enzyme inhibitor (arachidonate 5-lipoxygenase) or leukotriene receptor ...
Unlike common variants, mutations causing rare diseases tend to be in the regions of genes that encode proteins, providing both ... activated a system to isolate anyone diagnosed with the virus and to trace and quarantine all of their contacts. Iceland's ... 5, no 1 February 2011, pp. 50-65 On deCODE in the context of the new genomics: Davies, Kevin, The $1,000 Genome: The Revolution ... 5 January 2017 C Brownstein, et al., "If I knew then what I know now: The need for infrastructure to enable precision medicine ...
"Crystal structure of inhibitor-bound human 5-lipoxygenase-activating protein". Science. 317 (5837): 510-2. Bibcode:2007Sci... ... How FLAP activates 5-lipooxygenase is not completely understood, but there is a physical interaction between the two.[citation ... It is an integral protein within the nuclear membrane. FLAP is necessary in synthesis of leukotriene, which are lipid mediators ... Leukotrienes, which require the FLAP protein to be synthesized, have an established pathological role in allergic and ...
This protein is involved in the production of cysteinyl leukotrienes which are involved in inflammation, and AM-679 has anti- ... AM-679 is a drug which acts as a selective inhibitor of 5-Lipoxygenase-activating protein (FLAP). ... a potent FLAP inhibitor". Bioorganic & Medicinal Chemistry Letters. 20 (1): 213-7. doi:10.1016/j.bmcl.2009.10.131. PMID ... Part 2: 3-{5-((S)-1-Acetyl-2,3-dihydro-1H-indol-2-ylmethoxy)-3-tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-1H- ...
BLT2 receptors, similar to BLT1 receptors, are G protein coupled receptors that, when ligand-bound, activate G proteins that ... adenocarcinoma cells in culture was stimulated by 12-HETE and inhibited by a somewhat selective inhibitor of 12-lipoxygenase, ... "Induction of cyclooxygenase-2 by activated Ha-ras oncogene in Rat-1 fibroblasts and the role of mitogen-activated protein ... thereby activating calcium-activated intracellular signaling molecules; it also stimulates cells to activate Extracellular ...
... and/or 271 by Mitogen-activated protein kinases, S6 kinase, protein kinase A (PKA), protein kinase C, Cdc2, and/or a Ca2+/ ... neither LTB4 synthesis inhibitors (i.e. blockers of ALOX5 or LTA4 hydrolase) nor inhibitors of LTB4 receptors (BLT1 and BLT2) ... ALOX5 binds with the F actin-binding protein, coactin-like protein. Based on in vitro studies, this protein binding serves to ... This chemotactic factor stimulation concurrently causes the activation of mitogen-activated protein kinases (MAPK) which in ...
... activate cells by releasing the Gq alpha subunit and pertussis toxin-sensitive Gi alpha subunit from Heterotrimeric G proteins ... Fourie, A. M. (2009). "Modulation of inflammatory disease by inhibitors of leukotriene A4 hydrolase". Current Opinion in ... and lipoxygenase-derived eicosanoids". Drug Metabolism and Disposition. 39 (2): 180-90. doi:10.1124/dmd.110.035121. PMC 3033693 ... but also bound and was activated by a wide range of peptides, proteins, and other agents. BLT2 may ultimately prove to have ...
Huntingtin Interacting protein 1) Hsp70 Histactophilin Hsp90 Histidine rich protein II Hsp100 Inhibitor of apoptosis (IAP) ... p21-activated Kinase) Plectin p47PHOX Parvin (actopaxin) Prefoldin p53 PASK (Proline, Alanine rich Ste20 related Kinase) ... Actin-binding proteins (also known as ABPs) are proteins that bind to actin. This may mean ability to bind actin monomers, or ... This is a list of actin-binding proteins in alphabetical order. List: 0-9 A B C D E F G H I J K L M N O P Q R S T U V W x Y Z ...
Other lipoxygenases-8-LO, 12-LO and 15-LO-make other eicosanoid-like products. To act, 5-LO uses the nuclear-membrane enzyme 5- ... lipoxygenase-activating protein (FLAP), first to a hydroperoxyeicosatetraenoic acid (HPETE), then to the first leukotriene, LTA ... Increasing DGLA intake may allow DGLA to act as a competitive inhibitor of 2-series PGs and 4-series LTs and thus suppress ... Lipoxygenase oxidation removes no C=C double bonds and leads to the LK. After oxidation, the eicosanoids are further modified, ...
It can be activated at sites of tissue injury or sites of inflammation directly by endogenous mediators or indirectly as a ... TRPA1+protein,+human at the US National Library of Medicine Medical Subject Headings (MeSH) (CS1 maint: DOI inactive as of July ... While the earliest inhibitors, such as HC-030031, were lower potency (micromolar inhibition) and had limited TRPA1 specificity ... May 2013). "Systematic analysis of rat 12/15-lipoxygenase enzymes reveals critical role for spinal eLOX3 hepoxilin synthase ...
As such, inhibitors of FAAH lead to elevated anandamide levels and are being pursued for therapeutic use. Anandamide was first ... Endocannabinoid transporters for anandamide and 2-arachidonoylglycerol include the heat shock proteins (Hsp70s) and fatty acid ... "Exercise activates the endocannabinoid system". NeuroReport. 14 (17): 2209-2211. doi:10.1097/00001756-200312020-00015. PMID ... role of vanilloid receptors and lipoxygenases". The Journal of Neuroscience. 23 (10): 4127-4133. doi:10.1523/JNEUROSCI.23-10- ...
The protein biology approach to this research involved trying to map complex processes using limited samples, mainly of brain ... It has been widely cited and used to inform the development of BACE1 inhibitors as potential treatments. Stefansson and the ... Genes encode proteins, so identifying the genes and specific genetic variations that patients tended to share more often than ... Although publishing steadily, Stefansson was frustrated by the pace of progress and often by not knowing whether the proteins ...
... inhibitor of 12-lipoxygenase but not other human lipoxygenases. This effect could also have anti-inflammatory and anti- ... 15(S)-HpETE and 15(S)-HETE bind to and activate the G protein-coupled receptor, Leukotriene B4 receptor 2, i.e. BLT2. This ... 15-Lipoxygenase-2: Cells also used 15-lipoxygenase 2 (i.e. 15-LOX-2 or ALOX15B) to make 15(S)-HpETE and 15(S)-HETE. However ... 15-Lipoxygenase-1: Cells metabolize arachidonic acid with 15-lipoxygenase-1 (i.e., 15-LO-1, ALOX15) to form 15(S)-HpETE as a ...
Receptors that activate this pathway are mainly G protein-coupled receptors coupled to the Gαq subunit, including: 5-HT2 ... Huang W, Barrett M, Hajicek N, Hicks S, Harden TK, Sondek J, Zhang Q (February 2013). "Small molecule inhibitors of ... and the lipoxygenase pathway (producing leukotrienes (LTB4, LTC4, LTD4, LTE4)). The bacterial variant Clostridium perfringens ... In addition, calcium and DAG together work to activate protein kinase C, which goes on to phosphorylate other molecules, ...
Most sensitizing pro-inflammatory agents activate the phospholipase C pathway. Phosphorylation of TRPV1 by protein kinase C ... that serves as an anandamide reuptake inhibitor and COX inhibitor also serves as a potent TRPV1 agonist. The plant- ... May 2013). "Systematic analysis of rat 12/15-lipoxygenase enzymes reveals critical role for spinal eLOX3 hepoxilin synthase ... TRPV1 is activated by numerous agonists from natural sources. Agonists such as capsaicin and resiniferatoxin activate TRPV1 and ...
Meconium can also activate the coagulation cascade, production of platelet-activating factor (PAF) and other vasoactive ... However, COX inhibitors may induce peptic ulcers and cause hyperkalemia and hypernatremia. Additionally, COX inhibitors have ... Surfactant is synthesised by type II alveolar cells and is made of a complex of phospholipids, proteins and saccharides. It ... Arachidonic acid is metabolised, via cyclooxygenase (COX) and lipoxygenase, to various substances including prostaglandins and ...
... cyclic adenosine monophosphate response element-binding protein phosphorylation, and p38 mitogen-activated protein kinase ... Delta12-lipoxygenase, 12Delta-lipoxygenase, and C-12 lipoxygenase. ALOX12, often termed plate platelet-type 12-lipoxygenase, is ... A selective but not totally specific inhibitor of ALOX12 reduced the growth response of cultured human endothelial cells to ... ALOX12 (EC 1.13.11.31), also known as arachidonate 12-lipoxygenase, 12-lipoxygenase, 12S-Lipoxygenase, 12-LOX, and 12S-LOX is a ...
Kelavkar, U. P; Cohen, C (2004). "15-lipoxygenase-1 expression upregulates and activates insulin-like growth factor-1 receptor ... HODE directly activate human (but not mouse) GPR132 (G protein coupled receptor 132, also termed G2A) in Chinese hamster ovary ... Ruparel, Shivani; Green, Dustin; Chen, Paul; Hargreaves, Kenneth M (2012). "The Cytochrome P450 Inhibitor, Ketoconazole, ... 12-lipoxygenase, and 15-lipoxygenase-2, and selected metabolites of the latter lipoxygenases show no such association. ...
... structure of the catalytic domain of porcine leukocyte 12-lipoxygenasean with inhibitor UMich Orientation of Proteins in ... and thereby are key regulators in the formation of lipoxygenase-dependent metabolites. In addition, cells, when so activated, ... erythrocyte type 15-lipoxygenase (or 15-lipoxygenase, erythrocyte type), reticulocyte type 15-lipoxygenase (or 15-lipoxygenase ... LOX-DB - LipOXygenases DataBase Lipoxygenases iron-binding region in PROSITE PDB: 1YGE​ - structure of lipoxygenase-1 from ...
Therefore, helenalin can interact with proteins by forming covalent bonds to the thiol groups of cysteine-containing proteins/ ... In vitro, it is also a potent, selective inhibitor of human telomerase-which may partially account for its antitumor effects- ... Helenalin also suppresses essential immune functions, such as those mediated by activated CD4+ T-cells, by multiple mechanisms ... inhibitors of cellular metabolism". Science. 196 (4289): 533-6. Bibcode:1977Sci...196..533L. doi:10.1126/science.191909. PMID ...
... metabolites many of which act on cells by binding with and thereby activating specific and well-characterized receptor proteins ... Finally, there are relatively few metabolite-forming lipoxygenases and cyclooxygenases in the first and second pathways and ... certain proton pump inhibitor and antidepressant drugs.[unreliable source?] As indicated above, Cytochrome P450 reductase (POR ... Proteins and Proteomics. 1814 (1): 210-22. doi:10.1016/j.bbapap.2010.09.009. PMID 20869469. Moran, J. H.; Weise, R; Schnellmann ...
CysLTR1 is a G protein-coupled receptor that links to and when bound to its CysLT ligands activates the Gq alpha subunit and/or ... Haeggström JZ, Funk CD (October 2011). "Lipoxygenase and leukotriene pathways: biochemistry, biology, and roles in disease". ... and drug inhibitors of CysLTR1 block the in vivo and in vivo (animal model) growth of CRC cells and tumors, respectively. The ... Acting through these G proteins and their subunits, ligand-bound CysLTR1 activates a series of pathways that lead to cell ...
Cannabidiol, a FAAH inhibitor, increases levels in anandamide and may have antipsychotic effect; though results are mixed here ... The lipoxygenase-5 inhibitor minocycline has been seen to be marginally effective in halting schizophrenia progression. One of ... Okada, F.; Crow, T. J.; Roberts, G. W. (1990). "G-proteins (Gi, Go) in the basal ganglia of control and schizophrenic brain". ... Similarly, toxoplasmosis infection in the CNS (positively correlated to schizophrenia) activates inflammatory cascades, also ...
Linker of activated T cells, Lymphocyte cytosolic protein 2, MAP2, MAP3K1 MAP4K1, MED28, MST1R, MUC1, Mitogen-activated protein ... "Direct binding of the signal-transducing adaptor Grb2 facilitates down-regulation of the cyclin-dependent kinase inhibitor ... "Induced direct binding of the adapter protein Nck to the GTPase-activating protein-associated protein p62 by epidermal growth ... the guanine nucleotide exchange protein Sos and a 75-kDa protein that is a substrate for T cell antigen receptor-activated ...
White blood cells are activated by upregulation of integrin avidity, the lipoxygenase pathway and arachidonic acid metabolism. ... C5aR is a member of the G-protein-coupled receptor superfamily of proteins, predicted to have seven transmembrane helical ... The inhibitor of C5a that can block its effects would be helpful in medical applications. Another candidate is PMX53 or PMX205 ... C5a is a protein fragment released from cleavage of complement component C5 by protease C5-convertase into C5a and C5b ...
Squalene oxidation activates NF-κB (a protein complex) and consequently increases IL-1α levels. Additionally, squalene ... peroxisome proliferator-activated receptor modulators, and inhibitors of the stearoyl-CoA desaturase-1 enzyme are also a focus ... LTB4 promotes skin inflammation by acting on the peroxisome proliferator-activated receptor alpha (PPARα) protein. PPARα ... Once the light activates the sensitizing substance, this generates free radicals and reactive oxygen species in the skin, which ...
As such, inhibitors of FAAH lead to elevated anandamide levels and are being pursued for therapeutic use.[6][7] ... Endocannabinoid transporters for anandamide and 2-arachidonoylglycerol include the heat shock proteins (Hsp70s) and fatty acid ... role of vanilloid receptors and lipoxygenases". The Journal of Neuroscience. 23 (10): 4127-4133. doi:10.1523/JNEUROSCI.23-10- ... "Exercise activates the endocannabinoid system". NeuroReport. 14 (17): 2209-2211. doi:10.1097/00001756-200312020-00015. PMID ...
... p120 gtpase activating protein MeSH D12.776.402.300.700.500 - ras-GRF1 MeSH D12.776.402.300.700.700 - son of sevenless proteins ... wnt1 protein MeSH D12.776.624.664.700.978 - wnt2 protein MeSH D12.776.624.776.355.100 - cyclin-dependent kinase inhibitor p15 ... lipoxygenase MeSH D12.776.556.579.374.450.025 - arachidonate lipoxygenases MeSH D12.776.556.579.374.450.025.020 - arachidonate ... groel protein MeSH D12.776.602.500.500.100 - fusion proteins, bcr-abl MeSH D12.776.602.500.500.320 - fusion proteins, gag-onc ...
J Neurosci Res 24:558-566, 1989 Squinto SP, Braquet P, Block AL, Bazan NG: Platelet-activating factor activates HIV promoter in ... Research led by Bazan in 2015 also discovered a protein in the retina that is crucial for vision. Bazan and his colleagues ... NeuroReport 12:53-57, 2001 Bazan NG, Birkle DL, Reddy TS: Docosahexaenoic acid (22:6, n 3) is metabolized to lipoxygenase ... This included the finding that seizure-induced platelet-activating factor production activates gene expression, as well as a ...
... suppressed the release of IL-2 protein from mouse EL-4 T cells that had been stimulated with phorbol 12-myristate 13- ... Myricetin was identified as a competitive inhibitor of the reverse transcriptase of Rauscher murine leukemia virus and a ... Myricetin, along with other lipoxygenase- and cyclooxygenase-blocker flavonoids are seen to have significant anti-inflammatory ... collagen and platelet activating factor (PAF). It inhibited specific receptor binding of PAF in rabbit platelets. The compound ...
In 2012, salicylic acid was found to activate AMP-activated protein kinase, which has been suggested as a possible explanation ... Several COX-2 inhibitors, such as rofecoxib (Vioxx), have been withdrawn from the market, after evidence emerged that PTGS2 ... It is proposed that this aspirin-triggered transition of COX-2 from cyclooxygenase to lipoxygenase activity and the ... "The ancient drug salicylate directly activates AMP-activated protein kinase". Science. 336 (6083): 918-22. Bibcode:2012Sci... ...
"Expression of X-linked inhibitor of apoptosis protein in human prostate cancer specimens with and without neo-adjuvant hormonal ... and is activated manually by the patient through a switch implanted in the scrotum. The latter is considered the gold standard ... Also in trials for CRPC are : checkpoint inhibitor ipilimumab, CYP17 inhibitor galeterone (TOK-001), and immunotherapy PROSTVAC ... Transport protein ZIP1 is responsible for the transport of zinc into prostate cells. One of zinc's important roles is to change ...
One or both of these compounds stimulates cells by binding with and activating two G protein-coupled receptors, GPR31 and the ... ALOX15 (also termed arachidonate 15-lipoxygenase, 15-lipoxygenase-1, 15-LO-1, 15-LOX-1) is, like other lipoxygenases, a seminal ... an inhibitor of human platelet aggregation (see Dihydroxy-E,Z,E-PUFA). 5(S),15(S)-dihydroxy-6Z,8E,llE,13Z-eicosatetraenoic acid ... 15-lipoxygenase-2, 15-LOX-2, 15-LO-2, arachidonate 15-lipoxygenase type II, arachidonate 15-lipoxygenase, second type, and ...
Proto-Oncogene+Proteins+c-sis at the US National Library of Medicine Medical Subject Headings (MeSH) McKinnon RD, Matsui T, ... Wortmannin is a PI3K-specific inhibitor, and treatment of cells with Wortmannin in combination with PDGF resulted in enhanced ... However, comparing the signaling pathways between them reveals that the PI3K pathway is exclusively activated by PDGF, with EGF ... "12/15-Lipoxygenase Contributes to Platelet-derived Growth Factor-induced Activation of Signal Transducer and Activator of ...
Cells metabolize DHA by ALOX12, other lipoxygenase, (12/15-lipoxygenase in mice), or an unidentified pathway to a 13S,14S- ... an inhibitor of the action of pro-inflammatory cytokine, interleukin 1), annexin A1 (an inhibitor of formation of pro- ... by either activating or inhibiting cells through binding to and thereby activating or inhibiting the activation of specific ... Certain of these PUFA-cyclopentenones bind to the sulfur residues in the KEAP1 component of the KEAP1-NFE2L2 protein complex in ...
CysLTR2, similar to CysLTR1, is a G protein-coupled receptor that links to and when bound to its CysLT ligands activates the Gq ... "WikiGenes - Collaborative Publishing". Haeggström JZ, Funk CD (October 2011). "Lipoxygenase and leukotriene pathways: ... There are as yet no selective inhibitors of CysLTR2 that are in clinical use (see Clinical significance section below). However ... Acting through these G proteins and their subunits, ligand-bound CysLTR1 activates a series of pathways that lead to cell ...
In 2012, salicylic acid was found to activate AMP-activated protein kinase, which has been suggested as a possible explanation ... Several COX-2 inhibitors, such as rofecoxib (Vioxx), have been withdrawn from the market, after evidence emerged that PTGS2 ... It is proposed that this aspirin-triggered transition of COX-2 from cyclooxygenase to lipoxygenase activity and the ... May 2012). "The ancient drug salicylate directly activates AMP-activated protein kinase". Science. 336 (6083): 918-22. Bibcode: ...
The two LXBs also trigger activation of Suppressor of cytokine signaling proteins (see SOCS proteins) which, in turn, inhibit ... Wu L, Li HH, Wu Q, Miao S, Liu ZJ, Wu P, Ye DY (2015). "Lipoxin A4 Activates Nrf2 Pathway and Ameliorates Cell Damage in ... The double oxygenations may be conducted within a single cell type which possess ALOX5 and an enzyme with 15-lipoxygenase ... reactive oxygen species and expression of Cell adhesion molecules and increase production of the platelet inhibitor, PGI2 and ...
... a decrease in cAMP concentration by inhibition of adenylyl cyclase and a rise in the concentration of mitogen-activated protein ... A neuropharmacological study demonstrated that an inhibitor of FAAH (URB597) selectively increases anandamide levels in the ... showed an increase in the expression of transcripts encoding myelin basic protein, endoplasmic proteins, cytochrome oxidase, ... NADA activates the TRPV1 channel with an EC50 of approximately of 50 nM.[clarify] The high potency makes it the putative ...
"Probing conformational changes in lipoxygenases upon membrane binding: Fine-tuning by the active site inhibitor ETYA". Biochim ... 2013). "Dietary fish oil and DHA down-regulate antigen-activated CD4+ T-cells while promoting the formation of liquid-ordered ... 1986). "Estimation of the polarity of the protein interior by optical spectroscopy". Nature. 319 (6048): 70-73. Bibcode: ... 18 (5): 591-598. doi:10.1016/j.semcdb.2007.07.011. PMID 17728161. Bagatolli, L. A. (2006). "To see or not to see: lateral ...
SHANK proteins are scaffolding proteins at glutamatergic synapses crucial for synaptic development. The disruption of SHANK ... VPA is a weak HDAC inhibitor. The VPA model discerns the potential pathogenesis and mechanisms of action of ASD in animal ... Activates and Represses Transcription". Science. 320 (5880): 1224-1229. Bibcode:2008Sci...320.1224C. doi:10.1126/science. ... In a small clinical trial, beta hydroxybutyrate, a product of the ketogenic diet and inhibitor of class 1 HDACs, has shown ...
... but instead activate other receptors (e.g. peroxisome proliferator-activated receptors (PPAR)-α/γ, G-protein coupled receptors ... FAAH inhibitors are seen to both increase alcohol consumption (NAE 20:4; AEA) and prevent against oxidative stress caused by ... amines by the lipoxygenase pathway". European Journal of Biochemistry. 267 (7): 2000-7. doi:10.1046/j.1432-1327.2000.01203.x. ... An in vivo active NAPE-PLD inhibitor called LEI-401 was found to be CNS-active, and modulated NAE biosynthesis. It had similar ...
This ester gives trenbolone an activated elimination half-life of about 3 days. Trenbolone acetate, or trenbolone 17β-acetate, ... Sinnett-Smith PA, Dumelow NW, Buttery PJ (September 1983). "Effects of trenbolone acetate and zeranol on protein metabolism in ... and lipoxygenases (LOX) (also known as: EC 1.13.11.34, EC 1.13.11.33, etc.). The bradykinin peptide is well known to promote a ... a mechanism for ACE-inhibitor cough". Nature Medicine. 2 (7): 814-817. doi:10.1038/nm0796-814. PMID 8673930. S2CID 6040673. ...
This protein is involved in the production of cysteinyl leukotrienes which are involved in inflammation, and AM-679 has anti- ... AM-679 is a drug which acts as a selective inhibitor of 5-Lipoxygenase-activating protein (FLAP). ... a potent FLAP inhibitor". Bioorganic & Medicinal Chemistry Letters. 20 (1): 213-7. doi:10.1016/j.bmcl.2009.10.131. PMID ... Part 2: 3-{5-((S)-1-Acetyl-2,3-dihydro-1H-indol-2-ylmethoxy)-3-tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-1H- ...
PCSK9 protein inhibitor. Subcutaneous. Revacept. AdvanceCor. Phase II. Platelet membrane glycoprotein VI inhibitors ... Atuliflapon (formerly AZD 5718) is an orally available, small molecule, 5-lipoxygenase activating protein inhibitor, being ...
... inhibitors for the treatment of respiratory and cardiovascular disease. • Swiss-based Octapharma will relocate its US ...
Articles & Whitepapers, Structural Biology & Protein Science Binding and SAR of Direct Inhibitors of the Nrf2-Keap1 Complex. ... 12/15-Lipoxygenase as a Regulator of Axon Degeneration. * 2 March 2021 ... Previous Page1 Page2 Page3 Page4 Page5 Page6 Page7 Page8 Page9 Page10 Page11 Page12 Page13 Page14 Page15 Page16 Page17 Page18 ...
Another lipoxygenase inhibitor (AA861) also protected against Aβ and iron toxicity whereas the the 5-lipoxygenase-activating ... protein inhibitor L655,238 and the cyclooxygenase inhibitor indomethacin were ineffective. These findings suggest that NDGA can ... Another lipoxygenase inhibitor (AA861) also protected against Aβ and iron toxicity whereas the the 5-lipoxygenase-activating ... Another lipoxygenase inhibitor (AA861) also protected against Aβ and iron toxicity whereas the the 5-lipoxygenase-activating ...
The EP1 receptor, via an unclassified G protein, can activate the PLC-IP3-Ca2+ pathway. All human EP3 isoforms can activate Gi ... Selective inhibitors of COX-2 and deletion of the enzyme delay ulcer healing in rodents, but the impact of COX-2 inhibitors in ... Products of Lipoxygenases. LOXs are a family of non-heme iron-containing enzymes that catalyze the oxygenation of polyenic ... TPα and TPβ receptors couple via Gq and several other G proteins, to activate the PLC-IP3-Ca2+ pathway (Figure 33-4). ...
Macrocyclic Modalities for Modulation of Protein-Protein Interactions (OC06). Dr St phanie GUERET ASTRAZENECA MPI SATELLITE ... Novel Bacterial Topoisomerase Inhibitors (NBTI) with Potent Gram-Negative Activity (T05). Dr Cornelia ZUMBRUNN IDORSIA ... Dr Erik Hett received his Ph.D. from Harvard University in the lab of Dr Eric Rubin, studying protein-protein interactions ... First, in a startup company named PIQUR Therapeutics focusing on the discovery of new PI3K inhibitors and eventually at the ...
TRANSPORTER -, INHIBITOR AL17N8ZSWL PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR GAMMA TARGET -, AGONIST 3XC8GUZ6CB SULFASALAZINE ... 2-HYDROXY-5-((4-((2-PYRIDINYLAMINO)SULFONYL)PHENYL)AZO)BENZOIC ACID [WHO-IP] Source:. ... InChI=1S/C18H14N4O5S/c23-16-9-6-13(11-15(16)18(24)25)21-20-12-4-7-14(8-5-12)28(26,27)22-17-3-1-2-10-19-17/h1-11,23H,(H,19,22)(H ... Inhibition of arachidonate 5-lipoxygenase by sulfasalazine and its major metabolites was observed at higher concentrations (2-3 ...
Analogues of profen compounds were synthesised for evaluation as mycobacterial growth inhibitors. ... incorporating known pharmacophores for FLAP inhibitors and CRTh2 antagonists. Synthetic routes towards the target compounds ... An attractive novel dual target strategy was the inhibition of the 5-lipoxygenase activating protein (FLAP) and antagonism of ... was investigated in order to access novel alkaloid structures and identify new leads for mycobacterial growth inhibitors. ...
From 5 year Indian Visa to a Transit or an Emergency Indian Visa, Indian Visa Online is fulfilling every eVisa needs ... Atuliflapon (formerly AZD 5718) is an orally available, small molecule, 5-lipoxygenase activating protein inhibitor, being ...
Chitosan but not chitin activates the inflammasome by a mechanism dependent upon phagocytosis. J Biol Chem. 2011 Oct 14; 286(41 ... Lipoxygenase Inhibitors. *Monoamine Oxidase Inhibitors. *Nucleic Acid Synthesis Inhibitors. *Ornithine Decarboxylase Inhibitors ... Prolyl-Hydroxylase Inhibitors. *Protease Inhibitors. *Protein Kinase Inhibitors. *Protein Synthesis Inhibitors. *Proton Pump ... "Nucleic Acid Synthesis Inhibitors" is a descriptor in the National Library of Medicines controlled vocabulary thesaurus, MeSH ...
2019). Expressed proteins and activated pathways in conditioned embryo culture media from IVF patients are diverse according to ... as a new class of potential pancreatic lipase inhibitors Nat Prod Res 35:863-866 doi:10.1080/14786419.2019.1607337 ... 2.5 Establishment of protein-protein interaction (PPI) network. To interpret the interaction between target proteins, the ... Second, a protein-protein interaction (PPI) network was established. Core genes were selected using Cytoscape software plugin. ...
Rational design of the zonulin inhibitor AT1001 derivatives as potential anti SARS-CoV-2. Webmaster2022-11-16T14:06:27+01:00 ... Abstract A deep in silico investigation of various microsomal prostaglandin E2 synthase-1 (mPGES-1) protein systems is here ... Identification of 2,4-Dinitro-Biphenyl-Based Compounds as MAPEG Inhibitors Galleria Identification of 2,4-Dinitro-Biphenyl- ... Identification of 2,4-Dinitro-Biphenyl-Based Compounds as MAPEG Inhibitors. Webmaster2022-11-16T14:09:58+01:00Novembre 16th, ...
... recombinant proteins & enzymes, and other innovative research tools for studying Apoptosis, Metabolism, Cell Proliferation, ... Ubiquitin Activating Enzyme E1 Inhibitor(1). *Ubiquitin Ligase (E3) Inhibitors(10). *Ubiquitin Proteasome Pathway Inhibitors(46 ... Lactate Dehydrogenase (LDH) Inhibitors(3). *Lipase Inhibitors(3). *Lipoxygenase (LO) Inhibitors(9) ... Therefore PDE inhibitors are suggested to have great therapeutic value in the adjunctive therapy of Cancer. PDE inhibitors have ...
This protein localizes to the plasma membrane. Inhibitors of its function impede translocation of 5-lipoxygenase from the ... GO:0019372 [lipoxygenase pathway]. GO:0031965 [nuclear membrane]. GO:0043085 [positive regulation of catalytic activity]. GO: ... Protein evidence (Ezkurdia et al 2014). Protein evidence (Kim et al 2014). RAS pathway related proteins. Ribosomal proteins. ... The protein classes assigned to this protein are shown if expanding the data in the protein class column. Parent protein ...
Most of the existing 5-LOX inhibitors are synthetic and exhibit adverse side effects. In view of this, there is need to search ... 5-Lipoxygenase (5-LOX) plays an important role in the inflammation process by synthesizing leukotrienes and several lipid ... Therefore, the present study was carried out to screen the most potential 5-LOX inhibitors from essential oil components of ... The molecular dynamic results showed that these 4 phytoconstituents interacted stably with the 5-LOX active site residues and ...
Calcineurin Inhibitors. *Protein Phosphatase-2B Inhibitors. *Protein Phosphatase 2B Inhibitors. *Protein Phosphatase 3 ... Lipoxygenase Inhibitors. *Monoamine Oxidase Inhibitors. *Nucleic Acid Synthesis Inhibitors. *Ornithine Decarboxylase Inhibitors ... "Calcineurin Inhibitors" is a descriptor in the National Library of Medicines controlled vocabulary thesaurus, MeSH (Medical ... This graph shows the total number of publications written about "Calcineurin Inhibitors" by people in this website by year, and ...
Lipoxygenase Inhibitors. *Monoamine Oxidase Inhibitors. *Nucleic Acid Synthesis Inhibitors. *Ornithine Decarboxylase Inhibitors ... Prolyl-Hydroxylase Inhibitors. *Protease Inhibitors. *Protein Kinase Inhibitors. *Protein Synthesis Inhibitors. *Proton Pump ... Cytochrome P-450 Monooxygenase Inhibitors*Cytochrome P-450 Monooxygenase Inhibitors. *Cytochrome P 450 Monooxygenase Inhibitors ... This graph shows the total number of publications written about "Cytochrome P-450 Enzyme Inhibitors" by people in this website ...
Lipoxygenase Inhibitors. *Monoamine Oxidase Inhibitors. *Nucleic Acid Synthesis Inhibitors. *Ornithine Decarboxylase Inhibitors ... Prolyl-Hydroxylase Inhibitors. *Protease Inhibitors. *Protein Kinase Inhibitors. *Protein Synthesis Inhibitors. *Proton Pump ... "Cyclooxygenase Inhibitors" is a descriptor in the National Library of Medicines controlled vocabulary thesaurus, MeSH (Medical ... This graph shows the total number of publications written about "Cyclooxygenase Inhibitors" by people in this website by year, ...
Lipoxygenase inhibitors attenuate growth of human pancreatic cancer xenografts and induce apoptosis through the... ... proteins Bcl-2 and Mcl-1 was significantly decreased after LOX inhibitor treatment while that of the. proapoptotic protein bax ... 8 were activated after treatment, concomitant with cleavage of the capase-3 substrate poly(ADP-. ribose) polymerase. In vivo ... Lipoxygenase inhibitors attenuate growth of human pancreatic cancer xenografts and induce apoptosis. through the mitochondrial ...
Effects of 5-Lipoxygenase Activating Protein Inhibitor on Abnormal Alveolarization and Lung Development Induced by 85% Oxygen ...
ACE, angiotensin-converting enzyme; ADP, adenosine diphosphate; aPC, activated protein C; BK, bradykinin; ecNOS, endothelial ... obstruct access of the bulky side chains of COX-2 inhibitors. Figure modified with permission from Nature from protein ... lipoxygenases, and epoxygenases to form a mesmerizing array of biologically active products. The COX enzymes are bisfunctional ... All of these products activate G protein-coupled receptors; the phenotypes resulting from deletion of these receptors has ...
Factor V Inhibitor Plasma. Cat# MBS514047. Supplier: MyBiosource. Available at Gentaur Genprice in 5 to 7 Working Days. Place ... Other Names: [factor V precusor; Coagulation factor V; coagulation factor V; coagulation factor V; Activated protein C cofactor ... MBS514047 , Factor V Inhibitor Plasma MyBiosource Plasma MBS514047 , Factor V Inhibitor Plasma. (No reviews yet) Write a Review ... MBS9933460 , Rat Dual Specificity Mitogen-Activated Protein Kinase Kinase 4 (MAP2K4) ELISA Kit MyBiosource Elisa Kits ...
Protease Inhibitor Cocktail, EDTA- Free, 20 Tablets. Inhibitors , Protein Inhibitors , Protease Inhibitors ... Curcumin also inhibits glutathione S-transferase,induction of nitric oxide in activated macrophages and inhibits EGF-induced ... Also shown to be a p300/CREB-binding protein-specific inhibitor of histone acetyltransferase, inhibiting the acetylation of ... Curcumin is a cell-permeable, antioxidant that acts as a dual inhibitor of 5-lipoxygenase (IC= 8 M) and cyclooxygenase (IC= 52 ...
peroxide, H2O2) has an additive cytotoxic effect on murine, colorectal tumor cells (CT26). Protein kinase inhibitors from a ... were able to activate the capsaicin-activated channel in isolated membrane patches of sensory neurons. Of these compounds, 12-( ... defined various other endogenous agonists of TRPV1 and exhibited that several products of lipoxygenases (LOXs) ... A combined mix of both could improve the performance of particular protein kinase inhibitors [62]. ROS be a part of essential ...
diacylglycerol as activators of mitogen-activated protein kinase and cytosolic phospholipase A2 in human neutrophil priming. ... A beta-lactam inhibitor of cytosolic phospholipase A2 which acts in a competitive, reversible manner at the lipid/water ... 8(S)-hydroxyeicosatetraenoic acid is the lipoxygenase metabolite of arachidonic acid that regulates epithelial cell migration ... Granulocyte-macrophage colony-stimulating factor primes neutrophils by activating a pertussis toxin-sensitive G protein not ...
MDM2SNP309 does not associate with elevated MDM2 protein expression or breast cancer risk. Oncology 2008 Jun 74 (1-2): 84-87. ... of breast cancer associated with genetic polymorphisms in the promoters of the matrix metalloproteinase-2 and tissue inhibitor ... 5-lipoxygenase and 5-lipoxygenase-activating protein gene polymorphisms, dietary linoleic acid, and risk for breast cancer. ... World journal of oncology 2017 Oct 8 (5): 162-170. Goske Maruthi, Ramachander V R Vinish, Komaravalli Prasanna Latha, Rahman P ...
Prostaglandin synthetase inhibitors in the treatment of primary dysmenorrhea. Outcome trials reviewed. American journal of ... Fish oils inhibit endothelial cell production of platelet-derived growth factor-like protein. Science, 1988, 241(4864):453-6. ... At the end of each month, the girls were asked to assess 2 main symptoms, abdominal pain and low back pain, on a 5-category ... Pediatrics, 1981, 68(5):661-4.. *OConnell K, Davis AR, Westhoff C. Self-treatment patterns among adolescent girls with ...
Peroxisome proliferator-activated proteins (PPARs). Group of nuclear receptor proteins that function as transcription factors ... Clinical Associations and Classification of Immune Checkpoint Inhibitor-Induced Cutaneous Toxicities * Slugging: A TikTok ... Activator protein 1 (AP-1). Induced by pro-inflammatory signals of acne, this transcription factor plays multiple roles, ... Sterol response binding protein-1 (SREBP-1). Transcription factors that can stimulate sebaceous gland lipogenesis. ...
  • Also inhibits arachidonate 5-lipoxygenase (IC 50 = 16 nM). (bio-techne.com)
  • This protein is involved in the production of cysteinyl leukotrienes which are involved in inflammation, and AM-679 has anti-inflammatory effects in animal studies. (wikipedia.org)
  • Inflammation is caused by a cascade of events, one of which is the metabolism of arachidonic acid, that begins with oxidation by the enzyme 5-lipoxygenase. (plos.org)
  • 5-Lipoxygenase (5-LOX) plays an important role in the inflammation process by synthesizing leukotrienes and several lipid mediators and has emerged as a possible therapeutic target for treatment of inflammatory diseases such as asthma and rheumatoid arthritis. (plos.org)
  • The enzyme 5-lipoxygenase (5-LOX) catalyzes the oxidation of arachidonic acid, which in turn reacts with eicosapentanoic acid, resulting in the formation of leukotrienes, the chemical mediators of inflammation [ 3 ]. (plos.org)
  • NSAIDs, which include both traditional NSAIDs (tNSAIDs) and selective inhibitors of COX-2 and which are among the most commonly used drugs ( 5 ), relieve pain and inflammation by suppressing the COX function of PGHS and the consequent formation of PGE 2 ( 6 ) and prostacyclin (PGI 2 ) ( 7 ), but perhaps also of other prostanoids. (jci.org)
  • These results suggest that CS may aggravate lung inflammation by activating EOS which, in turn, release inflammatory mediators promoting inflammatory cell recruitment and lung remodeling. (ispub.com)
  • Eosinophils are particularly evident in chronic lung inflammation where their products appear to play roles both in bronchial hyper-responsiveness and in tissue remodeling, leading to compromised lung function [ 5 , 6 ]. (ispub.com)
  • Additionally, eosinophil cytoplasmic lipid bodies contain cyclooxygenases (COX), lipoxygenases, and phospholipase A2, all of which contribute to inflammation through their role in synthesis of proinflammatory eicosanoids [ 18 ]. (ispub.com)
  • However, conventionally used PLGA-based microparticles are degraded by non-specific hydrolysis and produce acidic degradation products that can exacerbate local inflammation [27] and activate autocatalytic degradation of the particles [28]. (justia.com)
  • IL-31 induces skin inflammation (5) and scratching, an itch-associated response (11). (medicaljournals.se)
  • In conclusion, 5-oxo-ETE induces pulmonary eosinophilia in Brown Norway rats, raising the possibility that it may be a physiological mediator of inflammation in asthma. (arctichealth.org)
  • Glucosamine has been shown to decrease high-sensitivity C-reactive protein (hsCRP) by 28% and PGE-M by 24% [5] - knocking down two major markers for inflammation. (priceplow.com)
  • Membrane lipids supply the substrate for the synthesis of eicosanoids and platelet-activating factor (PAF). (mhmedical.com)
  • Substantial reduction in risk of breast cancer associated with genetic polymorphisms in the promoters of the matrix metalloproteinase-2 and tissue inhibitor of metalloproteinase-2 genes. (cdc.gov)
  • Genes up-regulated in CD4 [GeneID=920] T cells activated by anti-CD3 and anti-CD28: IL-12 (2h) versus untreated (2h). (gsea-msigdb.org)
  • A phase degraded in protein of the genes for the digestion of Doctor of Philosophy in Nursing at Massey University, Palmerston North, New Zealand. (familie-vos.de)
  • Genes identified as encoding anti-microbial proteins can now be rapidly and precisely introduced into elite germplasm, creating novel pathogen resistant lines ( Shah, 1997 ). (ejbiotechnology.info)
  • An important part of the strategies designed to engineer increased resistance of plants to fungal diseases is the discovery and characterisation of plant antifungal proteins and the isolation of their encoding genes. (ejbiotechnology.info)
  • however, more plant defence genes were activated by S. graminum feeding than S. avenae feeding. (biomedcentral.com)
  • The transcript levels of genes encoding cell wall-modifying proteins were significantly increased after S. graminum feeding, but only a few of these genes were induced by S. avenae . (biomedcentral.com)
  • The expression profile of NICTABA after caterpillar feeding was recorded in local as well as in systemic leaves, and compared to the expression of several genes encoding defense proteins, and genes encoding a tobacco systemin and the allene oxide cyclase, an enzyme in JA biosynthesis. (ipb-halle.de)
  • The significant genes had promoters enriched for HOXD12, HOXC13, and RREB-1 protein transcription factor binding sites. (biomedcentral.com)
  • The significant genes were enriched for promoters with ZIC1 protein transcription factor binding sites. (biomedcentral.com)
  • Moreover, the functionally-enhanced MuRF1−/− hearts regulate genes related to transcription, homeobox proteins, and kinases/phosphorylation. (biomedcentral.com)
  • This work revealed 7 damaging single nucleotide variants in 7 genes, enormous amplification across numerous chromosomes, huge rearrangement on chromosome 12, the presence of a putative retrotransposon and 11 fusions among genes.Materials and Elys Inhibitors products Methods SamplesSamples have been acquired after written informed consent was obtained in compliance with, and approval by, the Mayo Clinic Institutional Evaluation Board. (5htreceptor.com)
  • Leukotrienes (LTs) are a class of potent biological inflammatory mediators derived from arachidonic acid through the 5-lipoxygenase pathway. (skintherapyletter.com)
  • Using this approach, we identified an exceptionally potent, orally active, neurotrophic molecule that facilitates memory in normal rodents, and prevents the loss of synaptic proteins and cognitive decline in a transgenic AD mouse model. (plos.org)
  • U73122 is a potent phospholipase C (PLC) inhibitor, which reduces agonist-induced Ca 2+ increases in platelets and PMN. (selleckchem.com)
  • Liproxstatin-1 is a potent ferroptosis inhibitor with an IC50 of 22 nM. (selleckchem.com)
  • Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM and displays high selectivity over other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO). (selleckchem.com)
  • Varespladib (LY315920) is a potent and selective human non-pancreatic secretory phospholipase A2 (hnsPLA) inhibitor with IC50 of 7 nM. (selleckchem.com)
  • It is a potent inhibitor of human neutrophil adhesion to biological surfaces as well as adhesion-dependent granule exocytosis and oxidative burst. (enzolifesciences.com)
  • Cysteinyl leukotrienes (CysLTs) are potent lipid inflammatory mediators synthesized from arachidonic acid, through the 5-lipoxygenase (5-LO) pathway. (web.app)
  • Pterostilbene is equally potent as resveratrol in inhibiting 12-O-tetradecanoyl phorbol-13-acetate activated NFκB, AP-1, COX-2, and iNOS in mouse epidermis. (sciendo.com)
  • MG-132 (Z-Leu-Leu-Leu-al) is a potent proteasome and calpain inhibitor with IC 50 s of 100 nM and 1.2 μM, respectively. (medchemexpress.com)
  • Doxorubicin hydrochloride is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC 50 s of 0.8 μM and 2.67 μM, respectively. (medchemexpress.com)
  • We have shown previously that the 5-lipoxygenase product 5-oxo-6,8, 11,14-eicosatetraenoic acid (5-oxo-ETE) is a highly potent eosinophil chemoattractant in vitro. (arctichealth.org)
  • Abiraterone (CB-7598) is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay. (selleckchem.com)
  • Apigenin (NSC 83244, LY 080400) is a potent P450 inhibitor for CYP2C9 with K i of 2 μM. (selleckchem.com)
  • Itraconazole (R 51211) is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent. (selleckchem.com)
  • Glucocorticoids induce apoptosis and are endogenous, potent COX-2 inhibitors. (avensonline.org)
  • Tesaglitazar is a dual peroxisome proliferator-activated receptor (PPAR) alpha/gamma agonist that is more potent on PPARγ than on PPARα, with EC50s of 13.4 μM and 3.6 μM for rat PPARα and human PPARα, respectively. (adooq.com)
  • 3.The higher the number of " * " is, the more potent the inhibitor or activator is. (adooq.cn)
  • ALK2-IN-2 is a potent and selective inhibitor of activin receptor-like kinase 2 (ALK2) with an IC50 of 9 nM, and over 700-fold selectivity against ALK3. (adooq.cn)
  • As a result, inhibition of 5-LOX enzymes has been established as a rational approach for developing novel anti-inflammatory drugs with a better safety profile. (plos.org)
  • commonly known as COX) enzymes, lipoxygenases, and epoxygenases to form a mesmerizing array of biologically active products. (jci.org)
  • The COX enzymes are bisfunctional proteins, possessing both COX and hydroperoxidase (HOX) activities, catalyzing the biotransformation of AA into the PG endoperoxide intermediates PGG 2 and PGH 2 . (jci.org)
  • With following highly we are - N-acetylneuraminic enzymes, proteins, alpha and surface, dyslexia, and Digestion - building autoreactivity suggests primarily we are. (erik-mill.de)
  • Although humans and other mammals can synthesize saturated fatty acids and some monounsaturated fatty acids from carbon groups in carbohydrates and proteins , they lack the delta (Δ) 12 and Δ15 desaturase enzymes necessary to insert a cis double bond at the n-6 or the n-3 position of a fatty acid (1) . (oregonstate.edu)
  • Hh recordkeeping has associated for a particle of hybrid Proteins, and tetramers that belong the 1-methyladenine sucrose and expression of Hh glutamate can signal in globular enzymes. (familie-vos.de)
  • Although the mechanism of action has not been fully elucidated, thimerosal inhibits sulfhydryl-containing active site of various enzymes and binds to sulfhydryl compounds, such as glutathione, cysteine, and SH groups of proteins. (medindex.am)
  • We propose that most of FT-related proteins are enzymes operating on small diffusible molecules. (biomedcentral.com)
  • The polygalacturonase-inhibiting proteins (PGIPs) are key members of a class of anti-fungal proteins that potently inhibit the activity of cell wall-degrading fungal enzymes ( De Lorenzo and Cervone, 1997 ). (ejbiotechnology.info)
  • Oxidative stress produces an increase in enzymes such as cyclooxygenase (COX) and lipoxygenase (LOX) which are implicated in the release of interleukins and chemokines, and it has been shown that Flavay ® inhibits these pro-inflammatory enzymes. (flavay.com)
  • Pioglitazone HCl (AD-4833, U-72107E) is an inhibitor of cytochrome P450 (CYP)2C8 and CYP3A4 enzymes. (selleckchem.com)
  • Decreasing the activity of proteins that increase the levels of fat-producing enzymes (C/EBP-α, PPAR -γ, SREBP1c , and aP2) [ 40 , 41 , 42 , 43 ]. (selfdecode.com)
  • Curcumin also inhibits glutathione S-transferase,induction of nitric oxide in activated macrophages and inhibits EGF-induced tyrosine phosphorylation of EGF receptors. (agscientific.com)
  • 5.?Non-cannabinoid receptor 1, non-cannabinoid receptor 2 g-protein-coupled receptors Some ECs ([64] defined various other endogenous agonists of TRPV1 and exhibited that several products of lipoxygenases (LOXs) were able to activate the capsaicin-activated channel in isolated membrane patches of sensory neurons. (alexjordan.org)
  • However, the cannabinoid and TRPV1 receptors belong to different families of proteins: CB1 and CB2 receptors are seven trans-membrane domain name and GPCRs [67], and TRPV1 receptors are six trans-membrane domain name cation channels of the large TRP superfamily and more specifically, the TRPV Stachyose tetrahydrate channel subfamily [68]. (alexjordan.org)
  • Molecules associated with microbial pathogens that are recognized by toll-like receptors and pattern recognition receptors and thus activate innate immune responses. (medscape.com)
  • transient receptor potential vanilloid type 1 channel (TRPV1), and peroxisome proliferator-activated receptor γ.9 The CB1 receptors are found throughout the central nervous system and concentrate in the cortex, basal ganglia, hippocampus, and cerebellum on axon terminals and preterminal axon segments. (secret-seeds.com)
  • The cause of androgenetic alopecia, therefore, should not be sought in the amount of DHT produced, but in the higher level of 5 alpha reductase and androgen receptors present in areas subject to androgenetic alopecia. (hair-army.com)
  • Several researches have been carried out on fruit extracts which show that Serenoa repens is very rich in active ingredients such as triglycerides, phytosterols, sitosterol derivatives, flavonoids that give it antiandrogenic properties, which it performs mainly through a direct action on dihydrotestosterone receptors (DHT ), ed indirectly, through the inhibition of the enzyme 5-alpha-reductase, which is why it is widely used in the treatment of androgenic alopecia. (hair-army.com)
  • They belong to the super family of G-protein coupled receptors (Sakurai T. et al. (justia.com)
  • Propylhexedrine binds to and activates alpha-adrenergic receptors in the mucosa of the respiratory tract, thereby mimicking the actions of norepinephrine and epinephrine. (medindex.am)
  • In the biosynthesis of leukotrienes, 5-LOX plays a critical role, and it is perceived that drugs that inhibit 5-LOX will inhibit the generation of inflammatory mediators from the arachidonic acid pathway. (plos.org)
  • Our previous studies have demonstrated that blockade of either the 5-lipoxygenase (LOX) or 12-LOX pathway of arachidonic acid metabolism inhibited pancreatic cancer cell proliferation and induced apoptosis. (cyclingforums.com)
  • In conclusion, LOX inhibitors block pancreatic cancer cell proliferation and induce apoptosis through the mitochondrial pathway both in vivo and in vitro. (cyclingforums.com)
  • In addition, XQLD also markedly attenuated endoplasmic reticulum stress (ERS) and activated AMPK/mTOR pathway in the lung tissues of mice with AECOPD. (hindawi.com)
  • miRNA-300/NAMPT inhibited inflammatory responses through activating AMPK/mTOR signaling pathway in neonatal sepsis [ 12 ]. (hindawi.com)
  • The cysteinyl leukotrienes (cys-LTs) are 5-lipoxygenase pathway products implicated in asthma, in particular, by their function as smooth muscle constrictors of airways and microvasculature. (web.app)
  • Baicalein can be discovered to repress development and promote apoptosis of many pancreatic cancers cell lines through preventing TAK-901 the 12-lipoxygenase pathway and activating the mitochondrion-dependent apoptotic pathway [14C16]. (tech-strategy.org)
  • There are two major pathways of apoptotic cell death induction: The intrinsic pathway, also called the Bcl-2-regulated or mitochondrial pathway, is activated by various developmental cues or cytotoxic insults, such as viral infection, DNA damage and growth-factor deprivation, and is strictly controlled by the BCL-2 family of proteins. (medchemexpress.com)
  • 11βHSD2 inhibition may represent a novel approach for CRC chemoprevention by increasing tumor cell intracellular glucocorticoid activity, which in turn inhibits tumor growth by suppressing the COX-2-derived PGE2 pathway, as well as other pathways, without potential side-effects relating to chronic application of COX-2 inhibitors, NSAIDs and glucocorticoids. (avensonline.org)
  • Dipeptidyl peptidase-4 inhibitors (DPP4I) inhibit the degradation of endogenous GLP-1 and various other active substances. (bmj.com)
  • PIAS proteins inhibit the activity of signal transducers and activators of transcription. (nih.gov)
  • Inhibits 5-lipoxygenase in vivo and in vitro (IC50 = 30nM for recombinant enzyme and 2.4µM for PMNL homogenates). (enzolifesciences.com)
  • Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl)pyrimidines. (vanderbilt.edu)
  • In vitro we exhibited that IL-5 stimulates the selective chemokinesis of bone tissue marrow eosinophils, an activity markedly inhibited by two structurally specific inhibitors of phosphatidylinositol 3-kinase, wortmannin and "type":"entrez-nucleotide","attrs":"text message":"LY294002″,"term_id":"1257998346″,"term_text message":"LY294002″LY294002. (careersfromscience.org)
  • Arachidonic acid is acted upon by the enzyme 5-lipoxygenase to synthesize LTB4and cysteinyl leukotrienes (cys-LT C4, D4, and E4). (web.app)
  • AM-679 is a drug which acts as a selective inhibitor of 5-Lipoxygenase-activating protein (FLAP). (wikipedia.org)
  • Amira Pharmaceuticals (San Diego, CA) and GlaxoSmithKline (Middlesex, United Kingdom) have agreed to develop, manufacture and commercialize 'FLAP' (5-lipoxygenase activating protein) inhibitors for the treatment of respiratory and cardiovascular disease. (pharmtech.com)
  • An attractive novel dual target strategy was the inhibition of the 5-lipoxygenase activating protein (FLAP) and antagonism of the prostaglandin D2 receptor CRTh2. (ucl.ac.uk)
  • A combination of GlaxoSmithKline and literature SAR studies were elaborated in the design of the target compounds, incorporating known pharmacophores for FLAP inhibitors and CRTh2 antagonists. (ucl.ac.uk)
  • Nucleic Acid Synthesis Inhibitors" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (umassmed.edu)
  • This graph shows the total number of publications written about "Nucleic Acid Synthesis Inhibitors" by people in this website by year, and whether "Nucleic Acid Synthesis Inhibitors" was a major or minor topic of these publications. (umassmed.edu)
  • Below are the most recent publications written about "Nucleic Acid Synthesis Inhibitors" by people in Profiles. (umassmed.edu)
  • Important anti-inflammatory mechanisms of Flavay ® are the inhibition of pro-inflammatory mediators including phospholipase A2, cyclooxygenase (COX-1 and COX-2), and lipoxygenase thereby reducing destructive ratios and concentrations of prostanoids, leukotrienes and thromboxanes. (flavay.com)
  • Above:) An important anti-inflammatory mechanism of Flavay ® is the inhibition of pro-inflammatory mediators including phospholipase A2, cyclooxygenase (COX-1 and COX-2), and lipoxygenase thereby reducing destructive ratios and concentrations of prostanoids, leukotrienes and thromboxanes (without the side effects common to NSAIDs). (flavay.com)
  • Darapladib (SB-480848) is a reversible lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with IC50 of 0.25 nM. (selleckchem.com)
  • U73122 significantly inhibits aggregation of human platelets induced by a variety of agonists, including collagen, thrombin, ADP, arachidonic acid, with IC50 of 1-5 μM. (selleckchem.com)
  • Nintedanib is a small molecule tyrosine-kinase inhibitor with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β, respectively. (absource.de)
  • On the 5 th subculture, U-83836E had an IC50 of 37.5 m mM, but the cytotoxic effects of U-74389G was less than in that of the primary culture. (drlauda.at)
  • Abiraterone Acetate (CB7630) is an acetate salt form of Abiraterone which is a steroidal cytochrome CYP17 inhibitor with IC50 of 72 nM in a cell-free assay. (selleckchem.com)
  • WY-135 is an ALK (IC50=1.4 nM) and ROS1 (IC50=1.1 nM) dual inhibitor. (adooq.cn)
  • This study investigated the underlying mechanisms for LOX inhibitor-induced apoptosis and the potential of LOX inhibitors as antipancreatic cancer agents using the athymic mice xenograft model. (cyclingforums.com)
  • Apoptosis of pancreatic cancer cells induced by LOX inhibitors (including the nonselective LOX inhibitor nordihydroguaiaretic acid, the 5-LOX inhibitor Rev-5901, and the 12-LOX inhibitor baicalein) was confirmed by growth inhibition, annexin V binding, and terminal deoxynucleotidyl transferase-mediated nick end labeling assay in MiaPaCa-2 and AsPC-1 human pancreatic cancer cells. (cyclingforums.com)
  • In vivo studies in the athymic mice xenograft model also confirmed the growth inhibitory effect and induction of apoptosis by these LOX inhibitors in pancreatic cancer. (cyclingforums.com)
  • Endoplasmic reticulum stress is due to the imbalance of unfolded or misfolded proteins caused by free radicals and hypoxia in endoplasmic reticulum lumen, which leads to the apoptosis of bronchial and alveolar epithelial cells. (hindawi.com)
  • Kidney and adipose protein levels of apoptosis-associated speck-like protein 1, NLRP3, TNFα and Caspase-1 were higher in the BTBR and Akita mice than in the WT mice. (bmj.com)
  • Included in this, inhibition of Akt signaling network marketing leads to reduced phosphorylation from the downstream mammalian focus on of rapamycin (mTOR) to arrest cell routine and induce cell apoptosis or autophagy [19C22], whereas ERK signaling suppression leads to downregulation of matrix metalloproteinases (MMPs) but upregulation from the tissues inhibitor of metalloproteinases (TIMPs) to lessen cell motility and migration [23, 24]. (tech-strategy.org)
  • Proteins that contain this domain play a role in APOPTOSIS-related signal transduction by associating with other CARD domain-containing members and in activating INITIATOR CASPASES that contain CARD domains within their N-terminal pro-domain region. (uams.edu)
  • neuroectodermal apoptosis is contained in a plasma of sugars binding to their cell, activating in transient ATPs rotting development, molecules, classification, step, kidney and single selection. (familie-vos.de)
  • Glutathione plays important roles in antioxidant defense, nutrient metabolism, and regulation of cellular events (including gene expression, DNA and protein synthesis, cell proliferation and apoptosis, signal transduction, cytokine production and immune response, and protein glutathionylation). (researchgate.net)
  • Glucocorticoids have been used to treat diseases caused by an overactive immune system, such as allergies, asthma, and autoimmune diseases as well as a broad spectrum of hematologic malignancies, including leukemia, lymphoma, and myeloma due to their ability to induce apoptosis [ 3-5 ]. (avensonline.org)
  • PDE inhibitors can prolong or enhance the effects of physiological processes mediated by cAMP or cGMP by inhibition of their degradation by PDE. (biovision.com)
  • However, recent reports have introduced substantial complexity disconnecting the LTA 4 H modulator 4-methoxydiphenylmethane (4MDM) from PGP as follows: (1) 4MDM inhibits PGP hydrolysis and subsequently inhibition of LTA 4 H AP activity, and (2) 4MDM activates the same enzyme target in the presence of alternative substrates. (nature.com)
  • Included in this, Baicalein (5,6,7-trihydroxyflavone) may be the most appealing component with a number of pharmaceutical results, such as for example antioxidation, antithrombosis, bacterias- and virus-killing properties, aswell as inhibition of inflammatory response and hypersensitive edema [7, 8]. (tech-strategy.org)
  • As shown in Figure 5, six MP transport was matter to competitive inhibition using a 100 fold concentration of non radiolabeled six MP. (kinasepathway.com)
  • In some cell types, activation of PKC and/or inhibition of certain phosphatases with okadaic acid also contribute to cPLA 2 activation [ 5 ]. (biomedcentral.com)
  • Incubation of cells with cycloheximide alone resulted in inhibition of mTOR protein suggesting a requirement for ongoing protein synthesis to sustain basal mTOR levels. (5htreceptor.com)
  • Halobetasol propionate is thought to act by the induction of phospholipase A2 (PLA2) inhibitory proteins. (selleckchem.com)
  • Coupled with influx of extracellular calcium, Rut produced the endothelium-dependent vasorelaxant effect by activation of endothelium NOS and release of NO without pertussis toxin-sensitive Gi protein and other G proteins or phospholipase C activation being involved [ 8 ]. (biomedcentral.com)
  • In the present study, the lipoxygenase inhibitor/antioxidant nordihydroguaiaretic acid (NDGA) protected cultured rat hippocampal neurons against the toxicity of Aβ in a concentration-dependent manner. (elsevier.com)
  • MyBiosourceProduct Short Name: [Coagulation Factor V Inhibitor Plasma]Product Name Synonyme: N/AOther Names: N/AProduct Gene Name: N/AProduct. (biocheminfo.org)
  • MyBiosourceProduct Short Name: [Coagulation Factor X Inhibitor Plasma, Severe]Product Name Synonyme: N/AOther Names: N/AProduct Gene. (biocheminfo.org)
  • 5-lipoxygenase and 5-lipoxygenase-activating protein gene polymorphisms, dietary linoleic acid, and risk for breast cancer. (cdc.gov)
  • 19, for motifs) by specific transporters signaling sites in IL12 molecules cause Ca2+-activated from KFT because the Direct gene of the transport course binds synaptic at oxidation. (erik-mill.de)
  • We showed in zebrafish embryos that the alpha-tocopherol transfer protein (TTP) gene (Ttpa) increases 7-fold by 12 hours post-fertilization (hpf) and remains elevated. (converia.de)
  • Finally, 5 DMRs were further validated that the genome-wide DNA data were reliable through PS-PCR and 5 DEGs were confirmed the relationship between DNA methylation and gene expression by qRT-PCR. (biomedcentral.com)
  • Searches for a diffusible hormone-like signaling entity ("florigen") went on for many decades, until a product of plant gene FT was identified as the key component of florigen in the 1990s, based on the analysis of mutants, genetic complementation evidence, and protein and RNA localization studies. (biomedcentral.com)
  • A polygalacturonase-inhibiting protein ( pgip ) gene from Malus domestica cv Granny Smith apple plants was cloned by degenerate oligo-primed polymerase chain reaction (PCR) and Inverse PCR. (ejbiotechnology.info)
  • A new set of PCR primers were designed to the 5' and 3' ends of the gene, which allowed amplification of the full-length gene from apple genomic DNA. (ejbiotechnology.info)
  • IL-5 induces eosinophilopoiesis, activation and chemotaxis. (skintherapyletter.com)
  • It induces eosinophil synthesis and release of IL-8, an important chemotactic and activating factor for neutrophils and lymphocytes [ 22 , 23 ] which induces adhesion molecule expression also triggers the oxidative burst response, contributing to tissue damage [ 24 ]. (ispub.com)
  • A recent study showed that IL-31 increases the intracellular Ca 2+ ion concentration in the primary cultures of mouse dorsal root ganglia (DRG) neurones, suggesting that IL-31 directly activates primary afferents and induces itch sensation (13). (medicaljournals.se)
  • S. graminum and S. avenae feeding induces the JA, SA and ET signalling pathways, but S. graminum activated stronger plant defence responses than S. avenae . (biomedcentral.com)
  • 5-oxo-ETE induces pulmonary eosinophilia in an integrin-dependent manner in Brown Norway rats. (arctichealth.org)
  • Unlike cigarette smoke exposure, LPS exposure does not suppress endogenous LTA 4 H AP activity, and therefore, active LTA 4 H AP clears PGP after exposure to LPS in murine lung 5 . (nature.com)
  • Lipoxins (LXs), endogenous lipoxygenase-derived eicosanoids, represent a unique class of lipid mediators that possess a wide spectrum of anti-inflammatory and pro-resolving actions. (biomedcentral.com)
  • However, there are only few data on NO, polymorphisms of endothelial NO synthase (eNOS) and endogenous inhibitors of eNOS in children with primary hypertension. (czytelniamedyczna.pl)
  • We discuss findings from studies evaluating polymorphisms of eNOS and especially of G894T polymorphism and endogenous inhibitors of eNOS in hypertensive children and children with cardiovascular risk factors. (czytelniamedyczna.pl)
  • The endogenous levels of abscisic acid (ABA) and jasmonic acid (JA) were analyzed in wheat seedlings grown in water, a system which in the past has been used to test the effects of these plant growth inhibitors. (usda.gov)
  • U73122 potently inhibits human 5-lipoxygenase (5-LO) . (selleckchem.com)
  • U-73122 (10 μM) inhibits the production of IP3 and the subsequent rapid increase in cytosolic Ca 2+ induced by either thrombin or U-46619 through inhibiting hydrolysis of phosphatidyl[ 3 H]inositol and phosphatldyl[ 3 H]inosito1 4,5-bisphosphate catalyzed by a soluble fraction from platelets (K i =9 and 40 μM, respectively). (selleckchem.com)
  • Bafilomycin A1 blocks autophagosome-lysosome fusion and inhibits acidification and protein degradation in lysosomes of cultured cells. (medchemexpress.com)
  • Erythromycin is a macrolide antibiotic that inhibits bacterial protein synthesis by binding to bacterial 50S ribosomal subunits and inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins. (absource.de)
  • not degraded as processive part, this expression acts the development protein with each additional activator described with a Activation to occur a func-tion amongst the musifications was. (evakoch.com)
  • It functions as an activator and inhibitor of sodium-coupled chloride co-transporters and as an inhibitor of potassium-coupled chloride co-transporters. (ucdenver.edu)
  • Several classes of drugs, most notably aspirin , the traditional non-steroidal anti-inflammatory agents (tNSAIDs), and the specific inhibitors of cyclooxygenase-2 (COX-2), such as the coxibs, owe their principal therapeutic effects to blockade of eicosanoid formation. (mhmedical.com)
  • Overproduction of mediators of the arachidonic acid (AA) cascade, particularly those of the cyclooxygenase (COX) and lipoxygenase (LOX) pathways, causes major inflammatory diseases in humans [ 2 ]. (plos.org)
  • monocyte chemoattractant protein 1 (MCP-1) and macrophage inflammatory protein-1α (MIP-1α) which are predominantly chemotactic for mononuclear leucocytes. (bmj.com)
  • The treatment necessary to recruit alveoli and prevent atelectasis in the immature lung may cause lung injury and activate the inflammatory cascade. (medscape.com)
  • The initial acute inflammatory reaction has an intrinsic function in healing tissue injury and plays an essential role in restoring tissue homeostasis [ 5 ]. (sciencemag.org)
  • This article reviews the anti-inflammatory relative and anti-infectious effects of Evodia rutaecarpa and its major bioactive components and the involvement of the nitric oxide synthases, cyclooxygenase, NADPH oxidase, nuclear factor kappa B, hypoxia-inducible factor 1 alpha, reactive oxygen species, prostaglandins, tumor necrosis factor, LIGHT, amyloid protein and orexigenic neuropeptides. (biomedcentral.com)
  • This process is self-propagating, as the ROS released by inflammatory cells can increase the expression of leukocyte adhesive factors on the endothelium, resulting in local extravasation of additional leukocytes that produce additional ROS [5, 6]. (justia.com)
  • By contrast, suppression of TRPV4 with a specific antagonist or in female Trpv4 KO mouse attenuated inflammatory cytokines and chemokines, prevented the degradation of tight junction proteins, and preserve blood-spinal cord barrier integrity, thereby attenuate the scarring after SCI. (jneurosci.org)
  • Although selective COX-2 inhibitors as well as non-steroidal anti-inflammatory drugs (NSAIDs) reduce the number and sizes of colonic adenomas, increased cardiovascular risks of selective COX-2 inhibitors and increased gastrointestinal side-effects of NSAIDs limit their use in chemoprevention of CRC. (avensonline.org)
  • Premier Joint & Disc is scientifically formulated to deliver an aggressive panel of clinically reviewed ingredients which contain powerful phytochemical compounds designed to directly promote a healthy inflammatory response by targeting key chemical signaling pathways that have the capacity to modulate pro-inflammatory cytokines and proteins associated with minor pain from everyday activities. (vitaminconcept.com)
  • The damage of healthy tissue leads to severe pain reactions in both acute and chronic inflammatory reactions [5,8]. (biomedres.us)
  • In the in vivo model rats, Turcuron restored the liver architecture and biochemical parameters and reduced the expression of inflammatory proteins in the liver. (phcog.com)
  • 7 Eosinophils secrete cytokines and mediators that injure tissue via reactive O2 intermediates and the release of toxic granule proteins. (skintherapyletter.com)
  • The download Global Environmental Assessments Information and and protein-coupled cell of citrate features the monoclonal of sequences in the partial complex, growing in PB1 tissue, repair and in nervous manifestations, potential member( Palacin et al. (evakoch.com)
  • Furthermore, both mRNA and protein degrees of NEDD9 are raised in pancreatic carcinoma weighed against the matched up adjacent noncancerous tissue [34, 35]. (tech-strategy.org)
  • A 2 integrinCblocking antibody markedly inhibited the mobilization of eosinophils from your bone tissue marrow activated by IL-5. (careersfromscience.org)
  • Wortmannin was also proven to stop eosinophil discharge induced Tozasertib by IL-5 in the perfused bone tissue marrow program. (careersfromscience.org)
  • To show chemokinesis of guinea pig bone tissue marrow eosinophils, IL-5 (0C3 nM) was put into the top and lower chambers inside a checkerboard design. (careersfromscience.org)
  • Description: This is Double-antibody Sandwich Enzyme-linked immunosorbent assay for detection of Human Calmodulin Like Protein 5 (CALML5) in Tissue homogenates, cell lysates and other biological fluids. (kits-elisa.com)
  • Description: Enzyme-linked immunosorbent assay based on the Double-antibody Sandwich method for detection of Human Calmodulin Like Protein 5 (CALML5) in samples from Tissue homogenates, cell lysates and other biological fluids with no significant corss-reactivity with analogues from other species. (kits-elisa.com)
  • even healthy tissue is always damaged [5]. (biomedres.us)
  • Because some breast cancers respond to estrogen, lowering estrogen production at the site of the cancer (i.e. the adipose tissue of the breast) with aromatase inhibitors has been proven to be an effective treatment for hormone-sensitive breast cancer in postmenopausal women. (mdwiki.org)
  • With the discovery of leptin in 1994 1 and the many other secreted proteins since that time, 2 the adipose tissue now is not only considered as an energy reservoir but has reached the status of a true endocrine organ. (clinicalgate.com)
  • Atuliflapon (formerly AZD 5718) is an orally available, small molecule, 5-lipoxygenase activating protein inhibitor, being developed by AstraZeneca. (brajnewsmagazine.org)
  • Another lipoxygenase inhibitor (AA861) also protected against Aβ and iron toxicity whereas the the 5-lipoxygenase-activating protein inhibitor L655,238 and the cyclooxygenase inhibitor indomethacin were ineffective. (elsevier.com)
  • Furthermore, a 5-lipoxygenase inhibitor (zileuton), but not a cyclooxygenase inhibitor (indomethacin), and a leuko-triene B 4 (LTB 4 ) receptor antagonist (CMHVA) attenuated the action of IL-31. (medicaljournals.se)
  • Synthesis, potency, and in vivo evaluation of 2-piperazin-1-ylquinoline analogues as dual serotonin reuptake inhibitors and serotonin 5-HT1A receptor antagonists. (jefferson.edu)
  • 5-Oxo-ETE-induced eosinophilia was unaffected by the LTB4 and PAF antagonists LY255283 and WEB 2170, respectively. (arctichealth.org)
  • Serum C reactive protein, tumor necrosis factor α (TNFα), interleukin (IL)-1β, IL-6 and IL-18 were significantly higher in the BTBR and Akita mice than in the WT mice. (bmj.com)
  • To understand the therapeutic potential of selective inhibitors of eicosanoid synthesis and action, we must first review the synthesis, metabolism, and mechanism of action of eicosanoids and PAF. (mhmedical.com)
  • Evidence from 2 randomized controlled-outcome trials (RCTs) of 2 structurally distinct selective inhibitors of COX-2 supports this hypothesis. (jci.org)
  • Mast cells (MCs) are activated in vivo during DENV infection, and we show that this elevates systemic levels of their vasoactive products, including chymase, and promotes vascular leakage. (elifesciences.org)
  • Eur J Herbal Med 1994;1:12-5. (drmyattswellnessclub.com)
  • Although NuMA is also a biosynthesis kinase channel of the L1 domain but also a receptor shown with macrophages at the brain activity, unknown face weapons of NuMA include associated activated that receptor with the alpha during function( Tang et al, 1994). (erik-mill.de)
  • Neural precursor cell portrayed developmentally downregulated 9 CR2 (NEDD9), also called as individual enhancer of filamentation 1 (HEF1) or Cas-L (Crk-associated substrate L), is normally a scaffold protein localized in focal adhesions to put together the focal adhesion kinase (FAK) as well as the non-receptor tyrosine kinase c-Src to modify multiple mobile signaling pathways [28, 29]. (tech-strategy.org)
  • This Cardiovascular virus of activated principles by DCs might be to their Cardiovascular growth for repair state( Monua & Trombetta. (evakoch.com)
  • As statins have a bone strengthening effect, combining a statin with an aromatase inhibitor could help prevent fractures and suspected cardiovascular risks, without potential of causing osteonecrosis of the jaw. (mdwiki.org)
  • Abstract A deep in silico investigation of various microsomal prostaglandin E2 synthase-1 (mPGES-1) protein systems is here reported using molecular dynamics (MD) simulations. (ebris.eu)
  • Inhibitors selective for prostaglandin G/H synthase-2 (PGHS-2) (known colloquially as COX-2) were designed to minimize gastrointestinal complications of traditional NSAIDs - adverse effects attributed to suppression of COX-1-derived PGE 2 and prostacyclin (PGI 2 ). (jci.org)
  • Pirinixic acid derivatives, a new class of drug candidates for a range of diseases, interfere with targets including PPARα, PPARγ, 5-lipoxygenase (5-LO), and microsomal prostaglandin and E2 synthase-1 (mPGES1). (oncotarget.com)
  • In the meantime, a substantial number of pirinixic acid derivatives were synthesized that interfere with targets including PPARα, PPARγ, 5-lipoxygenase (5-LO), cyclooxygenase (COX), microsomal prostaglandin E2 synthase-1 (mPGES1), and γ-secretase at varying potencies [ 3 - 8 ]. (oncotarget.com)
  • Furthermore, we downregulated ATR applying siRNA in HEK293 cells to figure out no matter whether etoposide induction of both mTOR protein and phosphorylation at Ser2481 had been dependent on ATR (Figure 2B). (5htreceptor.com)
  • Pirinixic acid (WY-14,643) was discovered as a peroxisome proliferator-activated receptor (PPAR)α agonist in 1974 [ 1 ] and is related to the fibrates that are in clinical use for the treatment of hypercholesterolemia and hypertriglyceridemia [ 2 ]. (oncotarget.com)
  • Pioglitazone HCl is also a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist with EC50 of 0.93 μM and 0.99 μM for human PPARγ and mouse PPARγ, respectively. (selleckchem.com)
  • The early phase is characterized by the activation of the complement system ( 4 , 5 , 6 , 7 ), mast cell degranulation, and the release of vasoactive proinflammatory mediators such as histamine, serotonin, and TNF-α leading to neutrophil recruitment ( 8 , 9 , 10 ). (aai.org)
  • The endoplasmic reticulum (ER) is central to many cellular functions and is responsible for protein folding and biosynthesis. (hindawi.com)
  • Several specific DMGs which participated in protein kinase, cell and organelle, flavonoid biosynthesis and transcription factor were further identified to be likely associated with soybean response to bean pyralid. (biomedcentral.com)
  • Abiraterone acetate is an oral androgen biosynthesis inhibitor. (selleckchem.com)
  • Abiraterone (CB-7598) is an androgen biosynthesis inhibitor. (selleckchem.com)
  • A family of intracellular signaling adaptor proteins that contain caspase activation and recruitment domains. (uams.edu)
  • In addition, thimerosal activates the InsP3 calcium channel on endoplasmic reticular membrane, thereby triggering the release of calcium from intracellular stores resulting in a calcium-induced calcium-influx of extracellular calcium. (medindex.am)
  • It means expressed subsequent bacteria small to 1980)The and later is IL18RAP to activate a download A New Heart and a New Soul: Ezekiel, the Exile and the Torah (JSOT Supplement) intracellular protein( Sims 2002, Sergi & Pentilla 2004, Alboni et al. (evakoch.com)
  • Importantly focusing on intracellular PRL-3 protein suppressed malignancy growth [21]. (healthdisparitiesks.org)
  • Background Resistance to tyrosine kinase inhibitors (TKIs) remains challenging in management of individuals with chronic myeloid leukemia (CML). (healthdisparitiesks.org)
  • Protein-tyrosine phosphatase of regenerating liver 3 (PRL-3 encoded by mRNA [18] and showed that PRL-3 acting like a downstream CTS-1027 target of the internal tandem duplication (ITD) of fms-like tyrosine kinase (FLT3) signaling was implicated in FLT3 CTS-1027 inhibitor therapy in acute myeloid leukemia (AML) [19]. (healthdisparitiesks.org)
  • They also found that mice deficient in mast cells did not show dengue-induced vascular leakage, and that wild-type animals treated with drugs that block the actions of proteins produced by these cells, showed less vascular leakage than controls. (elifesciences.org)
  • Drugs belonging to the group known as 5-alpha-reductase inhibitors are used for problems due to DHT. (hair-army.com)
  • In order not to incur the side effects of 5-alpha-reductase inhibitor drugs, it is possible to use alternative natural treatments with functions similar to Finasteride, but without the same side effects. (hair-army.com)
  • Aromatase inhibitors ( AIs ) are a class of drugs used in the treatment of breast cancer in postmenopausal women and in men, [1] [2] and gynecomastia in men. (mdwiki.org)
  • 3 We have also shown that the amounts of degranulated proteins of neutrophils such as human neutrophil lipocalin (HNL), neutrophil collagenase (MMP-8), and gelatinase B (MMP-9) are also significantly higher in the BAL fluid from these subjects. (bmj.com)
  • Supernatants from CSE-activated EOS were found to be significantly chemotactic for neutrophils. (ispub.com)
  • Their recruitment, growth and survival are supported by cytokines and chemokines such as granulocyte-macrophage colony stimulating factor (GM-CSF), and interleukins (IL)- 3 and -5 [ 1 , 2 , 3 , 4 ]. (ispub.com)
  • Either cytokines such as IL-2, or neurohormones, such as the pineal indole melatonin (MLT), may activate anticancer immunity. (drlauda.at)
  • The humoral immune system is the part of the immune system based on plasma proteins (antibodies, complement factors and cytokines) [2,3]. (biomedres.us)
  • DAB adaptor protein 2 [Source:HG. (gsea-msigdb.org)
  • CARD Signaling Adaptor Proteins" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (uams.edu)
  • Below are the most recent publications written about "CARD Signaling Adaptor Proteins" by people in Profiles over the past ten years. (uams.edu)
  • They contain pleckstrin homology and SH2 domains, through which they function as signal transducing adaptor proteins. (nih.gov)
  • Since 5-LO, mPGES1, PPARα, and PPARγ represent potential anti-cancer drug targets, we here investigated the effects of 39 pirinixic acid derivatives on prostate cancer (PC-3) and neuroblastoma (UKF-NB-3) cell viability and, subsequently, the effects of selected compounds on drug-resistant neuroblastoma cells. (oncotarget.com)
  • Few compounds affected cancer cell viability in low micromolar concentrations but there was no correlation between the anti-cancer effects and the effects on 5-LO, mPGES1, PPARα, or PPARγ. (oncotarget.com)
  • Analogues of profen compounds were synthesised for evaluation as mycobacterial growth inhibitors. (ucl.ac.uk)
  • The molecular dynamic results showed that these 4 phytoconstituents interacted stably with the 5-LOX active site residues and the important bonds that were observed in the initial ligand docked compounds did not alter during the course of simulation. (plos.org)
  • However, 5 RCTs of 3 structurally distinct inhibitors also indicate that such compounds elevate the risk of myocardial infarction and stroke. (jci.org)
  • Therefore the compounds are delivered to cells either after dissolving in organic solvents or complexing with serum proteins. (enzolifesciences.com)
  • Phytochemical study of methanolic extract of eaves yielded 16 phytochemicals, including 5 isoflavones (1-5), flavones (6-8), flavonol (9), pterocarpans (10-11), phenolic compounds (12 and 13), phytosterols (14 and 15), and a sugar alcohol (16). (stuartxchange.ph)
  • The effects of both compounds on cell proliferation were determined using 3-(4,5-dimethyl thiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) colorimetric assay. (drlauda.at)
  • Extracts from Garcinia cambogia and compounds from the fruit are best known for potentially lowering body weight, reducing appetite, and preventing obesity [ 4 , 5 , 6 , 7 ]. (selfdecode.com)
  • However, IL-31 receptor complex is expressed not only in DRG neurones, but also in several immune cells (e.g. activated monocytes, macrophages, eosinophils, and basophils) and keratinocytes (4). (medicaljournals.se)
  • Eosinophils were then counted in lung sections that had been immunostained with an antibody to eosinophil major basic protein. (arctichealth.org)
  • 5-Oxo-ETE induced a dramatic increase in the numbers of eosinophils (ED50, 2.5 microg) around the walls of the airways, which reached maximal levels (five times control levels) between 15 and 24 h after administration, and then declined. (arctichealth.org)
  • approximately, the protein in acid side is enzymatic and, First to the central membrane of the Hamiltonian diseases, so following. (erik-mill.de)
  • Stanford UniversityJay LeBoeuf is protein dyslexia, coupling, and loop in the hormones transport membrane. (erik-mill.de)
  • A membrane protein homologous to the ERM (Ezrin-Radixin-Moesin) family of cytoskeleton-associated proteins which regulate physical properties of membranes. (nih.gov)
  • ATP then activated the P2X7 receptor (P2X7R) that was necessary for a peak of plasma-membrane actin assembly within 5 to 10 seconds in P2X7R-expressing J774, RAW and primary macrophages. (biologists.com)
  • In advanced forms, such as aggressive SM and MCL, agents targeting MC proliferation such as kinase inhibitors may be provided. (springer.com)
  • Direct defences involve the production and accumulation of plant defensive chemicals, such as plant secondary metabolites (PSMs), proteinase inhibitors, polyphenol oxidases and other defensive proteins, which are induced by herbivory and reduce herbivore performance [ 3 , 4 ]. (biomedcentral.com)
  • A family of structurally related proteins that are constitutively expressed and that negatively regulate cytokine-mediated SIGNAL TRANSDUCTION PATHWAYS. (nih.gov)
  • F-9775A and F-9775B are cathepsin K inhibitors that arise from a chromatin remodelling deletant strain of are recognized to produce a variety of structurally complex secondary Prucalopride metabolites many of which have significant relevance to human health. (healthdisparitiesks.org)
  • Hinokitiol also reduced interferon gamma (IFN- γ ) secretion from ConA-activated T lymphocytes, as detected by an ELISA assay. (hindawi.com)
  • Description: A sandwich ELISA kit for detection of Mitogen Activated Protein Kinase 9 from Human in samples from blood, serum, plasma, cell culture fluid and other biological fluids. (scalegen.com)
  • Description: A competitive ELISA for quantitative measurement of Human Calmodulin like protein 5(CALML5) in samples from blood, plasma, serum, cell culture supernatant and other biological fluids. (kits-elisa.com)
  • Browse our antibodies, ELISA kits and proteins related to positive regulation of endopeptidase activity. (antikoerper-online.de)
  • Other trophic factors, such as IL-2, TNF-α, and granulocyte-macrophage stimulating factor, cause activated T cells to produce interferon-γ, TNF-α, and TNF-β, leading to stimulation of macrophages and further up-regulation of leukocyte adhesion molecules. (medscape.com)
  • On the other hand, an 4 integrin obstructing antibody increased the pace of Tozasertib eosinophil mobilization induced by IL-5. (careersfromscience.org)
  • Description: This is Double-antibody Sandwich Enzyme-linked immunosorbent assay for detection of Human Basic Salivary Proline Rich Protein 1 (PRB1) in saliva and other biological fluids. (lipidx.org)
  • [5] It is degraded primarily by the fatty acid amide hydrolase (FAAH) enzyme, which converts anandamide into ethanolamine and arachidonic acid. (wikipedia.org)
  • The effect of AA on ENaC is specific because neither 5,8,11,14-eicosatetraynoic acid (ETYA), a nonmetabolized analogue of AA, nor 11,14,17-eicosatrienoic acid mimicked the inhibitory effect of AA on ENaC. (rupress.org)
  • Most FT homologs are known to share a constellation of five charged residues, three of which, i.e., two histidines and an aspartic acid, are located at the rim of a well-defined cavity on the protein surface. (biomedcentral.com)
  • Treatment of flag leaves and ears of wheat plants with MJ (jasmonic acid methylester) (10(-5) and 10(-4) M) did not increase ethylene production, but it did accelerate senescence as indicated by the loss of chlorophyll. (usda.gov)
  • Fig. 1 Chemical structures of Prucalopride orsellinic acid (1) and F-9775A (2) and B (3) gerfelin (4) C-10-deoxy gerfelin (5) diorcinol (6). (healthdisparitiesks.org)
  • Bafilomycin A1, a macrolide antibiotic, is also used as an autophagy inhibitor at the late stage. (medchemexpress.com)
  • The autophagy inhibitor 3‑MA markedly reversed the anti‑cardiac hypertrophy effects of Res. (spandidos-publications.com)
  • LOX inhibitors also markedly induced the release of cytochrome c from mitochondria into the cytosol. (cyclingforums.com)
  • The cell cycle inhibitor p21, which belongs to the Cip/Kip family, interferes with cycling by inhibiting all cyclin-dependent kinases (CDKs) involved in the G1/S phase, thereby controlling cell proliferation and tumorigenesis in various cell types [ 4 ]. (hindawi.com)