Precursors in the biosynthesis of prostaglandins and thromboxanes from arachidonic acid. They are physiologically active compounds, having effect on vascular and airway smooth muscles, platelet aggregation, etc.
Enzyme complexes that catalyze the formation of PROSTAGLANDINS from the appropriate unsaturated FATTY ACIDS, molecular OXYGEN, and a reduced acceptor.
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.
Synthetic compounds that are analogs of the naturally occurring prostaglandin endoperoxides and that mimic their pharmacologic and physiologic activities. They are usually more stable than the naturally occurring compounds.
A saclike, glandular diverticulum on each ductus deferens in male vertebrates. It is united with the excretory duct and serves for temporary storage of semen. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
A group of physiologically active prostaglandin endoperoxides. They are precursors in the biosynthesis of prostaglandins and thromboxanes. The most frequently encountered member of this group is the prostaglandin H2.
Cell surface receptors that bind prostaglandins with high affinity and trigger intracellular changes which influence the behavior of cells. Prostaglandin receptor subtypes have been tentatively named according to their relative affinities for the endogenous prostaglandins. They include those which prefer prostaglandin D2 (DP receptors), prostaglandin E2 (EP1, EP2, and EP3 receptors), prostaglandin F2-alpha (FP receptors), and prostacyclin (IP receptors).
(11 alpha,13E,15S)-11,15-Dihydroxy-9-oxoprost-13-en-1-oic acid (PGE(1)); (5Z,11 alpha,13E,15S)-11,15-dihydroxy-9-oxoprosta-5,13-dien-1-oic acid (PGE(2)); and (5Z,11 alpha,13E,15S,17Z)-11,15-dihydroxy-9-oxoprosta-5,13,17-trien-1-oic acid (PGE(3)). Three of the six naturally occurring prostaglandins. They are considered primary in that no one is derived from another in living organisms. Originally isolated from sheep seminal fluid and vesicles, they are found in many organs and tissues and play a major role in mediating various physiological activities.
A cyclic endoperoxide intermediate produced by the action of CYCLOOXYGENASE on ARACHIDONIC ACID. It is further converted by a series of specific enzymes to the series 2 prostaglandins.
A constitutively-expressed subtype of prostaglandin-endoperoxide synthase. It plays an important role in many cellular processes.
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.
Cell surface proteins that bind THROMBOXANES with high affinity and trigger intracellular changes influencing the behavior of cells. Some thromboxane receptors act via the inositol phosphate and diacylglycerol second messenger systems.
An enzyme found predominantly in platelet microsomes. It catalyzes the conversion of PGG(2) and PGH(2) (prostaglandin endoperoxides) to thromboxane A2. EC 5.3.99.5.
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.
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.
A group of physiologically active prostaglandin endoperoxides. They are precursors in the biosynthesis of prostaglandins and thromboxanes. Most frequently encountered member of this group is the prostaglandin G2.
2-Octylcyclopentaneheptanoic acids. The family of saturated carbon-20 cyclic fatty acids that represent the parent compounds of the prostaglandins.
(9 alpha,11 alpha,13E,15S)-9,11,15-Trihydroxyprost-13-en-1-oic acid (PGF(1 alpha)); (5Z,9 alpha,11,alpha,13E,15S)-9,11,15-trihydroxyprosta-5,13-dien-1-oic acid (PGF(2 alpha)); (5Z,9 alpha,11 alpha,13E,15S,17Z)-9,11,15-trihydroxyprosta-5,13,17-trien-1-oic acid (PGF(3 alpha)). A family of prostaglandins that includes three of the six naturally occurring prostaglandins. All naturally occurring PGF have an alpha configuration at the 9-carbon position. They stimulate uterine and bronchial smooth muscle and are often used as oxytocics.
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)
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.
The principal cyclooxygenase metabolite of arachidonic acid. It is released upon activation of mast cells and is also synthesized by alveolar macrophages. Among its many biological actions, the most important are its bronchoconstrictor, platelet-activating-factor-inhibitory, and cytotoxic effects.
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.
An unstable intermediate between the prostaglandin endoperoxides and thromboxane B2. The compound has a bicyclic oxaneoxetane structure. It is a potent inducer of platelet aggregation and causes vasoconstriction. It is the principal component of rabbit aorta contracting substance (RCS).
Any of the ruminant mammals with curved horns in the genus Ovis, family Bovidae. They possess lachrymal grooves and interdigital glands, which are absent in GOATS.
Compounds obtained by chemical synthesis that are analogs or derivatives of naturally occurring prostaglandins and that have similar activity.
Structurally related forms of an enzyme. Each isoenzyme has the same mechanism and classification, but differs in its chemical, physical, or immunological characteristics.
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 stable, physiologically active compound formed in vivo from the prostaglandin endoperoxides. It is important in the platelet-release reaction (release of ADP and serotonin).
Artifactual vesicles formed from the endoplasmic reticulum when cells are disrupted. They are isolated by differential centrifugation and are composed of three structural features: rough vesicles, smooth vesicles, and ribosomes. Numerous enzyme activities are associated with the microsomal fraction. (Glick, Glossary of Biochemistry and Molecular Biology, 1990; from Rieger et al., Glossary of Genetics: Classical and Molecular, 5th ed)
Physiologically active compounds found in many organs of the body. They are formed in vivo from the prostaglandin endoperoxides and cause platelet aggregation, contraction of arteries, and other biological effects. Thromboxanes are important mediators of the actions of polyunsaturated fatty acids transformed by cyclooxygenase.
A naturally occurring prostaglandin that has oxytocic, luteolytic, and abortifacient activities. Due to its vasocontractile properties, the compound has a variety of other biological actions.
Physiologically active prostaglandins found in many tissues and organs. They show pressor activity, are mediators of inflammation, and have potential antithrombotic effects.
(13E,15S)-15-Hydroxy-9-oxoprosta-10,13-dien-1-oic acid (PGA(1)); (5Z,13E,15S)-15-hydroxy-9-oxoprosta-5,10,13-trien-1-oic acid (PGA(2)); (5Z,13E,15S,17Z)-15-hydroxy-9-oxoprosta-5,10,13,17-tetraen-1-oic acid (PGA(3)). A group of naturally occurring secondary prostaglandins derived from PGE; PGA(1) and PGA(2) as well as their 19-hydroxy derivatives are found in many organs and tissues.
A stable prostaglandin endoperoxide analog which serves as a thromboxane mimetic. Its actions include mimicking the hydro-osmotic effect of VASOPRESSIN and activation of TYPE C PHOSPHOLIPASES. (From J Pharmacol Exp Ther 1983;224(1): 108-117; Biochem J 1984;222(1):103-110)
Compounds that inhibit the action of prostaglandins.
Cell surface receptors which bind prostaglandins with a high affinity and trigger intracellular changes which influence the behavior of cells. Prostaglandin E receptors prefer prostaglandin E2 to other endogenous prostaglandins. They are subdivided into EP1, EP2, and EP3 types based on their effects and their pharmacology.
A prostaglandin that is a powerful vasodilator and inhibits platelet aggregation. It is biosynthesized enzymatically from PROSTAGLANDIN ENDOPEROXIDES in human vascular tissue. The sodium salt has been also used to treat primary pulmonary hypertension (HYPERTENSION, PULMONARY).
Large enzyme complexes composed of a number of component enzymes that are found in STREPTOMYCES which biosynthesize MACROLIDES and other polyketides.
The attachment of PLATELETS to one another. This clumping together can be induced by a number of agents (e.g., THROMBIN; COLLAGEN) and is part of the mechanism leading to the formation of a THROMBUS.
Unsaturated azacyclopropane compounds that are three-membered heterocycles of a nitrogen and two carbon atoms.
Very toxic industrial chemicals. They are absorbed through the skin, causing lethal blood, bladder, liver, and kidney damage and are potent, broad-spectrum carcinogens in most species.
A potent nitrofuran derivative tumor initiator. It causes bladder tumors in all animals studied and is mutagenic to many bacteria.
A subclass of cyclooxygenase inhibitors with specificity for CYCLOOXYGENASE-2.
An increase in the rate of synthesis of an enzyme due to the presence of an inducer which acts to derepress the gene responsible for enzyme synthesis.
The physiologically active and stable hydrolysis product of EPOPROSTENOL. Found in nearly all mammalian tissue.
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 prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Aspirin also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p5)
Non-nucleated disk-shaped cells formed in the megakaryocyte and found in the blood of all mammals. They are mainly involved in blood coagulation.
The rate dynamics in chemical or physical systems.
A subtype of prostaglandin E receptors that specifically couples to GS ALPHA GTP-BINDING PROTEIN SUBUNITS and subsequently activates ADENYLYL CYCLASES. The receptor may also signal through the activation of PHOSPHATIDYLINOSITOL 3-KINASE.
A subtype of prostaglandin E receptors that specifically couples to GS ALPHA GTP-BINDING PROTEIN SUBUNITS and subsequently activates ADENYLYL CYCLASES.
A class of enzymes that catalyze geometric or structural changes within a molecule to form a single product. The reactions do not involve a net change in the concentrations of compounds other than the substrate and the product.(from Dorland, 28th ed) EC 5.
A potent vasodilator agent that increases peripheral blood flow.
The innermost membranous sac that surrounds and protects the developing embryo which is bathed in the AMNIOTIC FLUID. Amnion cells are secretory EPITHELIAL CELLS and contribute to the amniotic fluid.
A group of compounds that contain the structure SO2NH2.
A subtype of prostaglandin E receptors that specifically couples to GTP-BINDING PROTEIN ALPHA SUBUNIT, GQ and the subsequently activates TYPE C PHOSPHOLIPASES. Additional evidence has shown that the receptor can act through a calcium-dependent signaling pathway.
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.
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.
Analogs or derivatives of prostaglandins E that do not occur naturally in the body. They do not include the product of the chemical synthesis of hormonal PGE.
RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.
A subtype of prostaglandin E receptors that specifically couples to GTP-BINDING PROTEIN ALPHA SUBUNIT, GI and subsequently inhibits ADENYLYL CYCLASES.
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.
Any of the processes by which nuclear, cytoplasmic, or intercellular factors influence the differential control of gene action in enzyme synthesis.
Proteins isolated from the outer membrane of Gram-negative bacteria.
Phospholipases that hydrolyze the acyl group attached to the 2-position of PHOSPHOGLYCERIDES.
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.
Chloro(7,12-diethenyl-3,8,13,17-tetramethyl-21H,23H-porphine-2,18-dipropanoato(4-)-N(21),N(22),N(23),N(24)) ferrate(2-) dihydrogen.
The color-furnishing portion of hemoglobin. It is found free in tissues and as the prosthetic group in many hemeproteins.
Catalyzes reversibly the oxidation of hydroxyl groups of prostaglandins.
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.
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.
A hemeprotein from leukocytes. Deficiency of this enzyme leads to a hereditary disorder coupled with disseminated moniliasis. It catalyzes the conversion of a donor and peroxide to an oxidized donor and water. EC 1.11.1.7.
Phospholipases that hydrolyze one of the acyl groups of phosphoglycerides or glycerophosphatidates.
Established cell cultures that have the potential to propagate indefinitely.
The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065)
The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.
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.
Analogs or derivatives of prostaglandins F that do not occur naturally in the body. They do not include the product of the chemical synthesis of hormonal PGF.
A subclass of eicosanoid receptors that have specificity for THROMBOXANE A2 and PROSTAGLANDIN H2.
Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed.
A somewhat heterogeneous class of enzymes that catalyze the transfer of alkyl or related groups (excluding methyl groups). EC 2.5.
Physiologically active prostaglandins found in many tissues and organs. They are potent pressor substances and have many other physiological activities.
Theoretical representations that simulate the behavior or activity of chemical processes or phenomena; includes the use of mathematical equations, computers, and other electronic equipment.
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.
The parts of a macromolecule that directly participate in its specific combination with another molecule.
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).
The art or process of comparing photometrically the relative intensities of the light in different parts of the spectrum.
Genetically engineered MUTAGENESIS at a specific site in the DNA molecule that introduces a base substitution, or an insertion or deletion.
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).
The nonstriated involuntary muscle tissue of blood vessels.
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.
An enzyme that converts UDP glucosamine into chitin and UDP. EC 2.4.1.16.
Conversion of an inactive form of an enzyme to one possessing metabolic activity. It includes 1, activation by ions (activators); 2, activation by cofactors (coenzymes); and 3, conversion of an enzyme precursor (proenzyme or zymogen) to an active enzyme.
A condition due to a dietary deficiency of ascorbic acid (vitamin C), characterized by malaise, lethargy, and weakness. As the disease progresses, joints, muscles, and subcutaneous tissues may become the sites of hemorrhage. Ascorbic acid deficiency frequently develops into SCURVY in young children fed unsupplemented cow's milk exclusively during their first year. It develops also commonly in chronic alcoholism. (Cecil Textbook of Medicine, 19th ed, p1177)
Electrophoresis in which a polyacrylamide gel is used as the diffusion medium.
A group of SESQUITERPENES and their analogs that contain a peroxide group (PEROXIDES) within an oxepin ring (OXEPINS).
Chromatography on thin layers of adsorbents rather than in columns. The adsorbent can be alumina, silica gel, silicates, charcoals, or cellulose. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
A nonsteroidal anti-inflammatory agent with analgesic properties used in the therapy of rheumatism and arthritis.
A non-steroidal anti-inflammatory agent with antipyretic and antigranulation activities. It also inhibits prostaglandin biosynthesis.
An excited state of molecular oxygen generated photochemically or chemically. Singlet oxygen reacts with a variety of biological molecules such as NUCLEIC ACIDS; PROTEINS; and LIPIDS; causing oxidative damages.
A plant species of the genus ARTEMISIA, family ASTERACEAE. It is the source of the antimalarial artemisinin (ANTIMALARIALS).
Ligases that catalyze the joining of adjacent AMINO ACIDS by the formation of carbon-nitrogen bonds between their carboxylic acid groups and amine groups.
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.
An NADPH-dependent enzyme that catalyzes the conversion of L-ARGININE and OXYGEN to produce CITRULLINE and NITRIC OXIDE.
The internal portion of the kidney, consisting of striated conical masses, the renal pyramids, whose bases are adjacent to the cortex and whose apices form prominent papillae projecting into the lumen of the minor calyces.
A diverse family of extracellular proteins that bind to small hydrophobic molecules. They were originally characterized as transport proteins, however they may have additional roles such as taking part in the formation of macromolecular complexes with other proteins and binding to CELL SURFACE RECEPTORS.
Enzymes of the isomerase class that catalyze reactions in which a group can be regarded as eliminated from one part of a molecule, leaving a double bond, while remaining covalently attached to the molecule. (From Enzyme Nomenclature, 1992) EC 5.5.
A CALCIUM-dependent, constitutively-expressed form of nitric oxide synthase found primarily in NERVE TISSUE.
A free radical gas produced endogenously by a variety of mammalian cells, synthesized from ARGININE by NITRIC OXIDE SYNTHASE. Nitric oxide is one of the ENDOTHELIUM-DEPENDENT RELAXING FACTORS released by the vascular endothelium and mediates VASODILATION. It also inhibits platelet aggregation, induces disaggregation of aggregated platelets, and inhibits platelet adhesion to the vascular endothelium. Nitric oxide activates cytosolic GUANYLATE CYCLASE and thus elevates intracellular levels of CYCLIC GMP.
The facilitation of a chemical reaction by material (catalyst) that is not consumed by the reaction.
A synthetic prostaglandin E analog that protects the gastric mucosa, prevents ulceration, and promotes the healing of peptic ulcers. The protective effect is independent of acid inhibition. It is also a potent inhibitor of pancreatic function and growth of experimental tumors.
Elements of limited time intervals, contributing to particular results or situations.
Enzymes from the transferase class that catalyze the transfer of acyl groups from donor to acceptor, forming either esters or amides. (From Enzyme Nomenclature 1992) EC 2.3.
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)
The physiological narrowing of BLOOD VESSELS by contraction of the VASCULAR SMOOTH MUSCLE.
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.
FATTY ACIDS in which the carbon chain contains one or more double or triple carbon-carbon bonds.
Enzymes that catalyze the synthesis of FATTY ACIDS from acetyl-CoA and malonyl-CoA derivatives.
Adenosine 5'-(trihydrogen diphosphate). An adenine nucleotide containing two phosphate groups esterified to the sugar moiety at the 5'-position.
Drugs that stimulate contraction of the myometrium. They are used to induce LABOR, OBSTETRIC at term, to prevent or control postpartum or postabortion hemorrhage, and to assess fetal status in high risk pregnancies. They may also be used alone or with other drugs to induce abortions (ABORTIFACIENTS). Oxytocics used clinically include the neurohypophyseal hormone OXYTOCIN and certain prostaglandins and ergot alkaloids. (From AMA Drug Evaluations, 1994, p1157)
Natural compounds containing alternating carbonyl and methylene groups (beta-polyketones), bioenergenetically derived from repeated condensation of acetyl coenzyme A via malonyl coenzyme A, in a process similar to fatty acid synthesis.
Analogs or derivatives of prostaglandin A that do not occur naturally in the body. They do not include the product of the chemical synthesis of hormonal PGA.
Agents used in the treatment of malaria. They are usually classified on the basis of their action against plasmodia at different stages in their life cycle in the human. (From AMA, Drug Evaluations Annual, 1992, p1585)
The yellow body derived from the ruptured OVARIAN FOLLICLE after OVULATION. The process of corpus luteum formation, LUTEINIZATION, is regulated by LUTEINIZING HORMONE.
Proteins prepared by recombinant DNA technology.
The major progestational steroid that is secreted primarily by the CORPUS LUTEUM and the PLACENTA. Progesterone acts on the UTERUS, the MAMMARY GLANDS and the BRAIN. It is required in EMBRYO IMPLANTATION; PREGNANCY maintenance, and the development of mammary tissue for MILK production. Progesterone, converted from PREGNENOLONE, also serves as an intermediate in the biosynthesis of GONADAL STEROID HORMONES and adrenal CORTICOSTEROIDS.
A CALCIUM-independent subtype of nitric oxide synthase that may play a role in immune function. It is an inducible enzyme whose expression is transcriptionally regulated by a variety of CYTOKINES.
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.
Single pavement layer of cells which line the luminal surface of the entire vascular system and regulate the transport of macromolecules and blood components.
Consists of a polypeptide chain and 4'-phosphopantetheine linked to a serine residue by a phosphodiester bond. Acyl groups are bound as thiol esters to the pantothenyl group. Acyl carrier protein is involved in every step of fatty acid synthesis by the cytoplasmic system.
The discharge of an OVUM from a rupturing follicle in the OVARY.
Enzymes of the isomerase class that catalyze the transfer of acyl-, phospho-, amino- or other groups from one position within a molecule to another. EC 5.4.
A nonapeptide hormone released from the neurohypophysis (PITUITARY GLAND, POSTERIOR). It differs from VASOPRESSIN by two amino acids at residues 3 and 8. Oxytocin acts on SMOOTH MUSCLE CELLS, such as causing UTERINE CONTRACTIONS and MILK EJECTION.
Duration of blood flow after skin puncture. This test is used as a measure of capillary and platelet function.
The hollow thick-walled muscular organ in the female PELVIS. It consists of the fundus (the body) which is the site of EMBRYO IMPLANTATION and FETAL DEVELOPMENT. Beyond the isthmus at the perineal end of fundus, is CERVIX UTERI (the neck) opening into VAGINA. Beyond the isthmi at the upper abdominal end of fundus, are the FALLOPIAN TUBES.
The chemical alteration of an exogenous substance by or in a biological system. The alteration may inactivate the compound or it may result in the production of an active metabolite of an inactive parent compound. The alterations may be divided into METABOLIC DETOXICATION, PHASE I and METABOLIC DETOXICATION, PHASE II.
A synthetic prostaglandin F2alpha analog. The compound has luteolytic effects and is used for the synchronization of estrus in cattle.
An enzyme of long-chain fatty acid synthesis, that adds a two-carbon unit from malonyl-(acyl carrier protein) to another molecule of fatty acyl-(acyl carrier protein), giving a beta-ketoacyl-(acyl carrier protein) with the release of carbon dioxide. EC 2.3.1.41.
Phosphoric or pyrophosphoric acid esters of polyisoprenoids.
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.
Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).
The degree of similarity between sequences of amino acids. This information is useful for the analyzing genetic relatedness of proteins and species.
Drugs used to cause constriction of the blood vessels.
A polymeric mixture of polyesters of phosphoric acid and phloretin. It blocks some cellular responses to prostaglandins.
An enzyme that catalyzes the transfer of glucose from ADPglucose to glucose-containing polysaccharides in 1,4-alpha-linkages. EC 2.4.1.21.
Degradation of CORPUS LUTEUM. In the absence of pregnancy and diminishing trophic hormones, the corpus luteum undergoes luteolysis which is characterized by the involution and cessation of its endocrine function.
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.
An analytical method used in determining the identity of a chemical based on its mass using mass analyzers/mass spectrometers.
Enzymes that catalyze the transfer of glucose from a nucleoside diphosphate glucose to an acceptor molecule which is frequently another carbohydrate. EC 2.4.1.-.
A nonapeptide messenger that is enzymatically produced from KALLIDIN in the blood where it is a potent but short-lived agent of arteriolar dilation and increased capillary permeability. Bradykinin is also released from MAST CELLS during asthma attacks, from gut walls as a gastrointestinal vasodilator, from damaged tissues as a pain signal, and may be a neurotransmitter.
Compounds based on imidazolidine dione. Some derivatives are ANTICONVULSANTS.
A genus of trees of the Myrtaceae family, native to Australia, that yields gums, oils, and resins which are used as flavoring agents, astringents, and aromatics.
The main trunk of the systemic arteries.
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.
A superfamily of hundreds of closely related HEMEPROTEINS found throughout the phylogenetic spectrum, from animals, plants, fungi, to bacteria. They include numerous complex monooxygenases (MIXED FUNCTION OXYGENASES). In animals, these P-450 enzymes serve two major functions: (1) biosynthesis of steroids, fatty acids, and bile acids; (2) metabolism of endogenous and a wide variety of exogenous substrates, such as toxins and drugs (BIOTRANSFORMATION). They are classified, according to their sequence similarities rather than functions, into CYP gene families (>40% homology) and subfamilies (>59% homology). For example, enzymes from the CYP1, CYP2, and CYP3 gene families are responsible for most drug metabolism.
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
Highly reactive molecules with an unsatisfied electron valence pair. Free radicals are produced in both normal and pathological processes. They are proven or suspected agents of tissue damage in a wide variety of circumstances including radiation, damage from environment chemicals, and aging. Natural and pharmacological prevention of free radical damage is being actively investigated.
An enzyme formed from PROTHROMBIN that converts FIBRINOGEN to FIBRIN.
A soluble factor produced by MONOCYTES; MACROPHAGES, and other cells which activates T-lymphocytes and potentiates their response to mitogens or antigens. Interleukin-1 is a general term refers to either of the two distinct proteins, INTERLEUKIN-1ALPHA and INTERLEUKIN-1BETA. The biological effects of IL-1 include the ability to replace macrophage requirements for T-cell activation.
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 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.
Systems of enzymes which function sequentially by catalyzing consecutive reactions linked by common metabolic intermediates. They may involve simply a transfer of water molecules or hydrogen atoms and may be associated with large supramolecular structures such as MITOCHONDRIA or RIBOSOMES.
A class of compounds composed of repeating 5-carbon units of HEMITERPENES.
Cell surface receptors for EPOPROSTENOL. They are coupled to HETEROTRIMERIC G-PROTEINS.
Transferases are enzymes transferring a group, for example, the methyl group or a glycosyl group, from one compound (generally regarded as donor) to another compound (generally regarded as acceptor). The classification is based on the scheme "donor:acceptor group transferase". (Enzyme Nomenclature, 1992) EC 2.
A family of enzymes accepting a wide range of substrates, including phenols, alcohols, amines, and fatty acids. They function as drug-metabolizing enzymes that catalyze the conjugation of UDPglucuronic acid to a variety of endogenous and exogenous compounds. EC 2.4.1.17.
The relationships of groups of organisms as reflected by their genetic makeup.
A phorbol ester found in CROTON OIL with very effective tumor promoting activity. It stimulates the synthesis of both DNA and RNA.
Compounds with a core of 10 carbons generally formed via the mevalonate pathway from the combination of 3,3-dimethylallyl pyrophosphate and isopentenyl pyrophosphate. They are cyclized and oxidized in a variety of ways. Due to the low molecular weight many of them exist in the form of essential oils (OILS, VOLATILE).
A class of enzymes that transfers substituted phosphate groups. EC 2.7.8.
A CALCIUM-dependent, constitutively-expressed form of nitric oxide synthase found primarily in ENDOTHELIAL CELLS.
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).
The mucous membrane lining of the uterine cavity that is hormonally responsive during the MENSTRUAL CYCLE and PREGNANCY. The endometrium undergoes cyclic changes that characterize MENSTRUATION. After successful FERTILIZATION, it serves to sustain the developing embryo.
An eicosanoid, derived from the cyclooxygenase pathway of arachidonic acid metabolism. It is a stable and synthetic analog of EPOPROSTENOL, but with a longer half-life than the parent compound. Its actions are similar to prostacyclin. Iloprost produces vasodilation and inhibits platelet aggregation.
An enzyme that, in the pathway of cholesterol biosynthesis, catalyzes the condensation of isopentenyl pyrophosphate and dimethylallylpyrophosphate to yield pyrophosphate and geranylpyrophosphate. The enzyme then catalyzes the condensation of the latter compound with another molecule of isopentenyl pyrophosphate to yield pyrophosphate and farnesylpyrophosphate. EC 2.5.1.1.
An element with atomic symbol O, atomic number 8, and atomic weight [15.99903; 15.99977]. It is the most abundant element on earth and essential for respiration.
A synthetic analog of natural prostaglandin E1. It produces a dose-related inhibition of gastric acid and pepsin secretion, and enhances mucosal resistance to injury. It is an effective anti-ulcer agent and also has oxytocic properties.
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.
Lipid-containing polysaccharides which are endotoxins and important group-specific antigens. They are often derived from the cell wall of gram-negative bacteria and induce immunoglobulin secretion. The lipopolysaccharide molecule consists of three parts: LIPID A, core polysaccharide, and O-specific chains (O ANTIGENS). When derived from Escherichia coli, lipopolysaccharides serve as polyclonal B-cell mitogens commonly used in laboratory immunology. (From Dorland, 28th ed)
A genus of OOMYCETES in the family Saprolegniaceae. It is a parasite and pathogen of freshwater FISHES.
Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding.
An enzyme that catalyzes the formation of riboflavin from two molecules of 6,7-dimethyl-8-ribityllumazine, utilizing a four-carbon fragment from one molecule which is transferred to the second molecule. EC 2.5.1.9.
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.
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 essential amino acid that is physiologically active in the L-form.
A genus of gram-positive bacteria whose spores are round to oval and covered by a sheath.
The increase in a measurable parameter of a PHYSIOLOGICAL PROCESS, including cellular, microbial, and plant; immunological, cardiovascular, respiratory, reproductive, urinary, digestive, neural, musculoskeletal, ocular, and skin physiological processes; or METABOLIC PROCESS, including enzymatic and other pharmacological processes, by a drug or other chemical.
The veins and arteries of the HEART.
The relatively long-lived phagocytic cell of mammalian tissues that are derived from blood MONOCYTES. Main types are PERITONEAL MACROPHAGES; ALVEOLAR MACROPHAGES; HISTIOCYTES; KUPFFER CELLS of the liver; and OSTEOCLASTS. They may further differentiate within chronic inflammatory lesions to EPITHELIOID CELLS or may fuse to form FOREIGN BODY GIANT CELLS or LANGHANS GIANT CELLS. (from The Dictionary of Cell Biology, Lackie and Dow, 3rd ed.)
Sets of enzymatic reactions occurring in organisms and that form biochemicals by making new covalent bonds.
Enzymes that catalyze the cleavage of a carbon-carbon bond of a 3-hydroxy acid. (Dorland, 28th ed) EC 4.1.3.
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.
Body organ that filters blood for the secretion of URINE and that regulates ion concentrations.
Lining of the STOMACH, consisting of an inner EPITHELIUM, a middle LAMINA PROPRIA, and an outer MUSCULARIS MUCOSAE. The surface cells produce MUCUS that protects the stomach from attack by digestive acid and enzymes. When the epithelium invaginates into the LAMINA PROPRIA at various region of the stomach (CARDIA; GASTRIC FUNDUS; and PYLORUS), different tubular gastric glands are formed. These glands consist of cells that secrete mucus, enzymes, HYDROCHLORIC ACID, or hormones.

Transformation of intestinal epithelial cells by chronic TGF-beta1 treatment results in downregulation of the type II TGF-beta receptor and induction of cyclooxygenase-2. (1/4015)

The precise role of TGF-beta in colorectal carcinogenesis is not clear. The purpose of this study was to determine the phenotypic alterations caused by chronic exposure to TGF-beta in non-transformed intestinal epithelial (RIE-1) cells. Growth of RIE-1 cells was inhibited by >75% following TGF-beta1 treatment for 7 days, after which the cells resumed a normal growth despite the presence of TGF-beta1. These 'TGF-beta-resistant' cells (RIE-Tr) were continuously exposed to TGF-beta for >50 days. Unlike the parental RIE cells, RIE-Tr cells lost contact inhibition, formed foci in culture, grew in soft agarose. RIE-Tr cells demonstrated TGF-beta-dependent invasive potential in an in vitro assay and were resistant to Matrigel and Na-butyrate-induced apoptosis. The RIE-Tr cells were also tumorigenic in nude mice. The transformed phenotype of RIE-Tr cells was associated with a 95% decrease in the level of the type II TGF-beta receptor (TbetaRII) protein, a 40-fold increase in cyclooxygenase-2 (COX-2) protein, and 5.9-fold increase in the production of prostacyclin. Most RIE-Tr subclones that expressed low levels of TbetaRII and high levels of COX-2 were tumorigenic. Those subclones that express abundant TbetaRII and low levels of COX-2 were not tumorigenic in nude mice. A selective COX-2 inhibitor inhibited RIE-Tr cell growth in culture and tumor growth in nude mice. The reduced expression of TbetaRII, increased expression of COX-2, and the ability to form colonies in Matrigel were all reversible upon withdrawal of exogenous TGF-beta1 for the RIE-Tr cells.  (+info)

Down-regulation of oxytocin-induced cyclooxygenase-2 and prostaglandin F synthase expression by interferon-tau in bovine endometrial cells. (2/4015)

Oxytocin (OT) is responsible for the episodic release of luteolytic prostaglandin (PG) F2alpha from the uterus in ruminants. The attenuation of OT-stimulated uterine PGF2alpha secretion by interferon-tau (IFN-tau) is essential for prevention of luteolysis during pregnancy in cows. To better understand the mechanisms involved, the effect of recombinant bovine IFN-tau (rbIFN-tau) on OT-induced PG production and cyclooxygenase-2 (COX-2) and PGF synthase (PGFS) expression in cultured endometrial epithelial cells was investigated. Cells were obtained from cows at Days 1-3 of the estrous cycle and cultured to confluence in RPMI medium supplemented with 5% steroid-free fetal calf serum. The cells were then incubated in the presence or absence of either 100 ng/ml OT or OT+100 ng/ml rbIFN-tau for 3, 6, 12, and 24 h. OT significantly increased PGF2alpha and PGE2 secretion at all time points (p < 0.01), while rbIFN-tau inhibited the OT-induced PG production and reduced OT receptor binding in a time-dependent manner. OT increased the steady-state level of COX-2 mRNA, measured by Northern blot, which was maximal at 3 h (9-fold increase) and then decreased with time (p < 0.01). OT also caused an increase in COX-2 protein, which peaked at 12 h (11-fold increase), as measured by Western blot. Addition of rbIFN-tau suppressed the induction of COX-2 mRNA (89%, p < 0.01) and COX-2 protein (50%, p < 0.01) by OT. OT also increased PGFS mRNA, and this stimulation was attenuated by rbIFN-tau (p < 0.01). To ensure that the decrease in COX-2 was not solely due to down-regulation of the OT receptor, cells were stimulated with a phorbol ester (phorbol 12-myristate 13-acetate; PMA) in the presence and absence of rbIFN-tau. The results showed that rbIFN-tau also decreased PMA-stimulated PG production and COX-2 protein. It can be concluded that rbIFN-tau inhibition of OT-stimulated PG production is due to down-regulation of OT receptor, COX-2, and PGFS.  (+info)

Mechanisms of prostaglandin E2 release by intact cells expressing cyclooxygenase-2: evidence for a 'two-component' model. (3/4015)

Prostaglandin (PG) release in cells expressing constitutive cyclooxygenase-1 is known to be regulated by liberation of arachidonic acid by phospholipase A2 followed by metabolism by cyclooxygenase. However, the relative contribution of phospholipase A2 to the release of PGs in cells expressing cyclooxygenase-2 is not clear. We addressed this question by using radioimmunoassay to measure PGE2 release by human cells (A549) induced to express cyclooxygenase-2 (measured by Western blot analysis) by interleukin-1beta. Cells were either unstimulated or stimulated with agents known to activate phospholipase A2 (bradykinin, Des-Arg10-kallidin, or the calcium ionophore A23187) or treated with exogenous arachidonic acid. When cells were treated to express cyclooxygenase-2, the levels of PGE2 released over 15 min were undetectable; however, in the same cells stimulated with bradykinin, A23187, or arachidonic acid, large amounts of prostanoid were produced. Using selective inhibitors/antagonists, we found that the effects of bradykinin were mediated by B2 receptor activation and that prostanoid release was due to cyclooxygenase-2, and not cyclooxygenase-1, activity. In addition, we show that the release of PGE2 stimulated by either bradykinin, A23187, or arachidonic acid was inhibited by the phospholipase A2 inhibitor arachidonate trifluoromethyl ketone. Hence, we have demonstrated that PGE2 is released by two components: induction of cyclooxygenase-2 and supply of substrate, probably via activation of phospholipase A2. This is illustrated in A549 cells by a clear synergy between the cytokine interleukin-1beta and the kinin bradykinin.  (+info)

Inhibition of prostaglandin synthesis up-regulates cyclooxygenase-2 induced by lipopolysaccharide and peroxisomal proliferators. (4/4015)

Primary cultures of fetal hepatocytes expressed cyclooxygenase-2 (COX-2) upon stimulation with bacterial lipopolysaccharide (LPS) or peroxisomal proliferators. This enzyme was active and a good correlation between the mRNA levels, the amount of protein, and the synthesis of prostaglandin E2 was observed. However, when cells were incubated in the presence of indomethacin or the COX-2-specific inhibitor NS398, the amount of COX-2 protein increased 5-fold after activation with LPS and 2-fold after treatment with clofibrate. This up-regulation of COX-2 was not observed at the mRNA level. The mechanism of protein accumulation might involve either a direct stabilization of the enzyme by the inhibitors or the absence of prostaglandins involved in the regulation of its turnover. Among the prostaglandins assayed, only 15-deoxy-Prostaglandin J2 exerted a statistically significant decrease in the COX-2 levels in cells stimulated with LPS or LPS plus NS398. The accumulation of COX-2 in the presence of inhibitors was also observed in peritoneal macrophages treated under identical conditions. These results indicate that COX-2 protein accumulates after enzyme inhibition, and because removal of the inhibitors restored the enzyme activity, suppression of treatment with reversible COX-2 inhibitors may cause a transient overproduction of prostaglandins.  (+info)

Characterization of the analgesic and anti-inflammatory activities of ketorolac and its enantiomers in the rat. (5/4015)

The marked analgesic efficacy of ketorolac in humans, relative to other nonsteroidal anti-inflammatory drugs (NSAIDs), has lead to speculation as to whether additional non-NSAID mechanism(s) contribute to its analgesic actions. To evaluate this possibility, we characterized (R,S)-ketorolac's pharmacological properties in vivo and in vitro using the nonselective cyclooxygenase (COX) inhibitors [indomethacin (INDO) and diclofenac sodium (DS)] as well as the selective COX-2 inhibitor, celecoxib, as references. The potency of racemic (R,S)-ketorolac was similar in tests of acetic acid-induced writhing, carrageenan-induced paw hyperalgesia, and carrageenan-induced edema formation in rats; ID50 values = 0.24, 0. 29, and 0.08 mg/kg, respectively. (R,S)-ketorolac's actions were stereospecific, with (S)-ketorolac possessing the biological activity of the racemate in the above tests. The analgesic potencies for (R,S)-, (S)-, and (R)-ketorolac, INDO, and DS were highly correlated with their anti-inflammatory potencies, suggesting a common mechanism. (R,S)-ketorolac was significantly more potent than INDO or DS in vivo. Neither difference in relative potency of COX inhibition for (R,S)-ketorolac over INDO and DS nor activity of (S)-ketorolac at a number of other enzymes, channels, or receptors could account for the differences in observed potency. The distribution coefficient for (R,S)-ketorolac was approximately 30-fold less than for DS or INDO, indicating that (R,S)-ketorolac is much less lipophilic than these NSAIDs. Therefore, the physicochemical and pharmacokinetics properties of (R,S)-ketorolac may optimize the concentrations of (S)-ketorolac at its biological target(s), resulting in greater efficacy and potency in vivo.  (+info)

The cyclo-oxygenase-dependent regulation of rabbit vein contraction: evidence for a prostaglandin E2-mediated relaxation. (6/4015)

1. Arachidonic acid (0.01-1 microM) induced relaxation of precontracted rings of rabbit saphenous vein, which was counteracted by contraction at concentrations higher than 1 microM. Concentrations higher than 1 microM were required to induce dose-dependent contraction of vena cava and thoracic aorta from the same animals. 2. Pretreatment with a TP receptor antagonist (GR32191B or SQ29548, 3 microM) potentiated the relaxant effect in the saphenous vein, revealed a vasorelaxant component in the vena cava response and did not affect the response of the aorta. 3. Removal of the endothelium from the venous rings, caused a 10 fold rightward shift in the concentration-relaxation curves to arachidonic acid. Whether or not the endothelium was present, the arachidonic acid-induced relaxations were prevented by indomethacin (10 microM) pretreatment. 4. In the saphenous vein, PGE2 was respectively a 50 and 100 fold more potent relaxant prostaglandin than PGI2 and PGD2. Pretreatment with the EP4 receptor antagonist, AH23848B, shifted the concentration-relaxation curves of this tissue to arachidonic acid in a dose-dependent manner. 5. In the presence of 1 microM arachidonic acid, venous rings produced 8-10 fold more PGE2 than did aorta whereas 6keto-PGF1alpha and TXB2 productions remained comparable. 6. Intact rings of saphenous vein relaxed in response to A23187. Pretreatment with L-NAME (100 microM) or indomethacin (10 microM) reduced this response by 50% whereas concomitant pretreatment totally suppressed it. After endothelium removal, the remaining relaxing response to A23187 was prevented by indomethacin but not affected by L-NAME. 7. We conclude that stimulation of the cyclo-oxygenase pathway by arachidonic acid induced endothelium-dependent, PGE2/EP4 mediated relaxation of the rabbit saphenous vein. This process might participate in the A23187-induced relaxation of the saphenous vein and account for a relaxing component in the response of the vena cava to arachidonic acid. It was not observed in thoracic aorta because of the lack of a vasodilatory receptor and/or the poorer ability of this tissue than veins to produce PGE2.  (+info)

Oxidative bioactivation of the lactol prodrug of a lactone cyclooxygenase-2 inhibitor. (7/4015)

The lactol derivative of a lactone cyclooxygenase-2 inhibitor (DFU) was evaluated in vivo and in vitro for its potential suitability as a prodrug. DFU-lactol was found to be 10 to 20 times more soluble than DFU in a variety of aqueous vehicles. After administration of DFU-lactol at 20 mg kg-1 p.o. in rats, a Cmax of 7.5 microM DFU was reached in the plasma. After oral administration, the ED50s of DFU-lactol in the carrageenan-induced paw edema and lipopolysaccharide-induced pyresis assays in rats are comparable with the ED50s observed when dosing with DFU. Incubations of DFU-lactol with rat and human hepatocytes demonstrated that the oxidation of DFU-lactol can be mediated by liver enzymes and that a competing pathway is direct glucuronidation of the DFU-lactol hydroxyl group. Assays with subcellular fractions from rat liver indicated that most of the oxidation of DFU-lactol occurs in the cytosolic fraction and requires NAD(P)+. Human liver cytosol can also support the oxidation of DFU-lactol to DFU when NAD(P)+ is added to the incubations. Fractionation of human liver cytosolic proteins showed that at least three enzymes are capable of efficiently effecting the oxidation of DFU-lactol to DFU. Incubations with commercially available dehydrogenases suggest that alcohol and hydroxysteroid dehydrogenases are involved in this oxidative process. These data together suggest that lactols may represent useful prodrugs for lactone-containing drugs.  (+info)

Coexistence of mitochondrial DNA and beta myosin heavy chain mutations in hypertrophic cardiomyopathy with late congestive heart failure. (8/4015)

OBJECTIVE: To investigate the possible coexistence of mitochondrial DNA (mtDNA) mutations in patients with beta myosin heavy chain (beta MHC) linked hypertrophic cardiomyopathy (HCM) who develop congestive heart failure. DESIGN: Molecular analysis of beta MHC and mtDNA gene defects in patients with HCM. SETTING: Cardiovascular molecular diagnostic and heart transplantation reference centre in north Italy. PATIENTS: Four patients with HCM who underwent heart transplantation for end stage heart failure, and after pedigree analysis of 60 relatives, eight additional affected patients and 27 unaffected relatives. A total of 111 unrelated healthy adult volunteers served as controls. Disease controls included an additional 27 patients with HCM and 102 with dilated cardiomyopathy. INTERVENTION: Molecular analysis of DNA from myocardial and skeletal muscle tissue and from peripheral blood specimens. MAIN OUTCOME MEASURES: Screening for mutations in beta MHC (exons 3-23) and mtDNA tRNA (n = 22) genes with denaturing gradient gel electrophoresis or single strand conformational polymorphism followed by automated DNA sequencing. RESULTS: One proband (kindred A) (plus seven affected relatives) had arginine 249 glutamine (Arg249Gln) beta MHC and heteroplasmic mtDNA tRNAIle A4300G mutations. Another unrelated patient (kindred B) with sporadic HCM had identical mutations. The remaining two patients (kindred C), a mother and son, had a novel beta MHC mutation (lysine 450 glutamic acid) (Lys450Glu) and a heteroplasmic missense (T9957C, phenylalanine (Phe)-->leucine (Leu)) mtDNA mutation in subunit III of the cytochrome C oxidase gene. The amount of mutant mtDNA was higher in the myocardium than in skeletal muscle or peripheral blood and in affected patients than in asymptomatic relatives. Mutations were absent in the controls. Pathological and biochemical characteristics of patients with mutations Arg249Gln plus A4300G (kindreds A and B) were identical, but different from those of the two patients with Lys450Glu plus T9957C(Phe-->Leu) mutations (kindred C). Cytochrome C oxidase activity and histoenzymatic staining were severely decreased in the two patients in kindreds A and B, but were unaffected in the two in kindred C. CONCLUSIONS: beta MHC gene and mtDNA mutations may coexist in patients with HCM and end stage congestive heart failure. Although beta MHC gene mutations seem to be the true determinants of HCM, both mtDNA mutations in these patients have known prerequisites for pathogenicity. Coexistence of other genetic abnormalities in beta MHC linked HCM, such as mtDNA mutations, may contribute to variable phenotypic expression and explain the heterogeneous behaviour of HCM.  (+info)

BioAssay record AID 162654 submitted by ChEMBL: Inhibitory activity against human recombinant Prostaglandin G/H synthase 2 expressed in microsomes taken from baculovirus infected Sf9 cells.
ptgs2, cox-2, cox2, gripghs, hcox-2, pgg/hs, pghs-2, phs-2; prostaglandin-endoperoxide synthase 2 (prostaglandin G/H synthase and cyclooxygenase); K11987 prostaglandin-endoperoxide synthase 2 [EC:1.14.99.1] ...
MAA699Hu22, PGG/HS; PGHS2; PHS2; HCox2; COX2; Cyclooxygenase 2; Prostaglandin G/H Synthase And Cyclooxygenase; Prostaglandin H2 synthase 2 | Products for research use only!
Because the levels of PGI synthase are comparable in the two muscle layers and do not vary with steroid treatments, it is tempting to conclude that the
Description: Enzyme-linked immunosorbent assay based on the Double-antibody Sandwich method for detection of Human Prostaglandin Endoperoxide Synthase 2 (PTGS2) in samples from serum, plasma, tissue homogenates and other biological fluids with no significant corss-reactivity with analogues from other species ...
Prostaglandin endoperoxide synthase 2, also referred to as cyclooxygenase 2 (COX-2), is a key enzyme in the conversion of arachidonic acid to prostaglandins and other eicosanoids. Rat intestinal epithelial (RIE) cells were permanently transfected with a COX-2 expression vector oriented in the sense …
Cyclooxygenase 1 (COX-1), also known as prostaglandin G/H synthase 1, prostaglandin-endoperoxide synthase 1 or prostaglandin H2 synthase 1, is an enzyme that in humans is encoded by the PTGS1 gene. In humans it is one of two cyclooxygenases. Cyclooxygenase (COX) is the central enzyme in the biosynthetic pathway to prostaglandins from arachidonic acid. This protein was purified more than 20 years ago and cloned in 1988. There are two isozymes of COX encoded by distinct gene products: a constitutive COX-1 (this enzyme) and an inducible COX-2, which differ in their regulation of expression and tissue distribution. The expression of these two transcripts is differentially regulated by relevant cytokines and growth factors. This gene encodes COX-1, which regulates angiogenesis in endothelial cells. COX-1 is also involved in cell signaling and maintaining tissue homeostasis. A splice variant of COX-1 termed COX-3 was identified in the CNS of dogs, but does not result in a functional protein in humans. ...
Cyclooxygenase (COX), officially known as prostaglandin-endoperoxide synthase (PTGS), is an enzyme (specifically, a family of isozymes) that is responsible for formation of prostanoids, including thromboxane and prostaglandins such as prostacyclin, from arachidonic acid. A member of the animal-type heme peroxidase family, it is also known as prostaglandin G/H synthase. The specific reaction catalyzed is the conversion from arachidonic acid to Prostaglandin H2, via a short-living Prostaglandin G2 intermediate ...
TY - JOUR. T1 - A new concept of the significance of regional distribution of prostaglandin H synthase 2 throughout the uterus during late pregnancy. T2 - Investigations in a baboon model. AU - Wu, W. X.. AU - Ma, X. H.. AU - Smith, G. C.S.. AU - Koenen, S. V.. AU - Nathanielsz, P. W.. PY - 2000/1/1. Y1 - 2000/1/1. N2 - OBJECTIVE: We sought to identify regional differences in prostaglandin H synthase 2 messenger ribonucleic acid expressions in various intrauterine tissues in the pregnant baboon as an indicator of prostaglandin production capability to explain the various interactive roles of different intrauterine tissues in the processes that precede, promote, and complete labor. STUDY DESIGN: Prostaglandin H synthase 2 messenger ribonucleic acid expression was measured by reverse transcriptase-polymerase chain reaction or Northern blot analysis in the uterine fundus, lower uterine segment, cervix, amnion, chorion, and placenta during late pregnancy and spontaneous term labor in the pregnant ...
Cyclooxygenase2 (COX-2), an inducible prostaglandin G/H synthase, is overexpressed in several human cancers. Here, the potential utility of selective COX-2 inhibitors in the prevention and treatment of cancer is considered. The mechanisms by which COX-2 levels increase in cancers, key data that indi …
Prostaglandin G/H synthase (PGHS), a key enzyme leading to the formation of prostaglandins, is the target of nonsteroidal antiinflammatory drugs. Two forms of the enzyme have been identified, PGHS-1 and PGHS-2. Epidemiological evidence has suggested that aspirin and other nonsteroidal antiinflammatory drugs may reduce the risk of colorectal cancer. We examined by immunoblot analyses the expression of human PGHS-1 and PGHS-2 protein in 25 matched colon cancer and nontumor tissues, 4 premalignant polyps, 5 control colon tissues from noncancer patients, and 3 matched normal and cancerous breast tissue samples. PGHS-1 was detected in all normal and tumor tissue. In contrast, PGHS-2 was not detected in 23 of 25 normal colon tissues but was detected in 19 of 25 colon tumors. PGHS-2 protein was not observed in four human premalignant polyp samples, control colon from noncancer patients, or matched normal or cancerous breast tissues. These results suggest that the beneficial effects of nonsteroidal ...
We investigated the mechanisms by which inhibitors of prostaglandin G/H synthase-2 (PGHS-2; known colloquially as COX-2) increase… Expand ...
Cyclooxygenase (COX, also called Prostaglandin H Synthase or PGHS) is a bifunctional enzyme exhibiting both COX and peroxidase activities. The COX component conv...
Looking for online definition of prostaglandin endoperoxide synthase in the Medical Dictionary? prostaglandin endoperoxide synthase explanation free. What is prostaglandin endoperoxide synthase? Meaning of prostaglandin endoperoxide synthase medical term. What does prostaglandin endoperoxide synthase mean?
Accepted name: prostaglandin-endoperoxide synthase. Reaction: arachidonate + reduced acceptor + 2 O2 = prostaglandin H2 + acceptor + H2O. Other name(s): prostaglandin synthase; prostaglandin G/H synthase; (PG)H synthase; PG synthetase; prostaglandin synthetase; fatty acid cyclooxygenase; prostaglandin endoperoxide synthetase. Systematic name: (5Z,8Z,11Z,14Z)-icosa-5,8,11,14-tetraenoate,hydrogen-donor:oxygen oxidoreductase. Comments: This enzyme acts both as a dioxygenase and as a peroxidase.. Links to other databases: BRENDA, EXPASY, KEGG, Metacyc, PDB, CAS registry number: 39391-18-9. References:. 1. DeWitt, D.L. and Smith, W.L. Primary structure of prostaglandin G/H synthase from sheep vesicular gland determined from the complementary DNA sequence. Proc. Natl. Acad. Sci. USA 85 (1988) 1412-1416. [PMID: 3125548]. 2. Ohki, S., Ogino, N., Yamamoto, S. and Hayaishi, O. Prostaglandin hydroperoxidase, an integral part of prostaglandin endoperoxide synthetase from bovine vesicular gland microsomes. ...
Prostaglandin-endoperoxide synthase (PTGS), also known as cyclooxygenase, is the key enzyme in prostaglandin biosynthesis, and acts both as a dioxygenase and as a peroxidase. There are two isozymes of PTGS: a constitutive PTGS1 and an inducible PTGS2, which differ in their regulation of expression and tissue distribution. This gene encodes the inducible isozyme. It is regulated by specific stimulatory events, suggesting that it is responsible for the prostanoid biosynthesis involved in inflammation and mitogenesis. [provided by RefSeq, Feb 2009 ...
Gallic acid esters possessing a varying chain length of their alcohol moiety were tested for their inhibitory potencies on 15-lipoxygenase from rabbit reticulocytes and prostaglandin H synthase from sheep vesicular glands. Octyl gallate and decyl gal
PTGS2 (COX-2) is unexpressed under normal conditions in most cells, but elevated levels are found during inflammation. PTGS1 (COX-1) is constitutively expressed in many tissues and is the predominant form in gastric mucosa and in the kidneys. Inhibition of PTGS1 (COX-1) reduces the basal production of cytoprotective PGE2 and PGI2 in the stomach, which may contribute to gastric ulceration. Since PTGS2 (COX-2) is generally expressed only in cells where prostaglandins are upregulated (e.g., during inflammation), drug-candidates that selectively inhibit PTGS2 (COX-2) were suspected to show fewer side-effects[25] but proved to substantially increase risk for cardiovascular events such as heart attack and stroke. Two different mechanisms may explain contradictory effects. Low-dose aspirin protects against heart attacks and strokes by blocking PTGS1 (COX-1) from forming a prostaglandin called thromboxane A2. It sticks platelets together and promotes clotting; inhibiting this helps prevent heart ...
Mono- and Stereopictres of 5.0 Angstrom coordination sphere of Cobalt atom in PDB 1diy: Crystal Structure Of Arachidonic Acid Bound in the Cyclooxygenase Active Site of Pghs-1
bom:102287995 K00509 prostaglandin-endoperoxide synthase 1 [EC:1.14.99.1] , (RefSeq) PTGS1; prostaglandin-endoperoxide synthase 1 (A) MSRQGISLRFPLLLLLLSPSPVLPADPGAPAPVNPCCYYPCQHQGICVRFGLDRYQCDCT RTGYSGPNCTIPEIWTWLRTTLRPSPSFVHFLLTHGRWLWDFVNATFIRDTLMRLVLTVR SNLIPSPPTYNIAHDYISWESFSNVSYYTRILPSVPRDCPTPMGTKGKKQLPDAEFLSRR FLLRRKFIPDPQGTNLMFAFFAQHFTHQFFKTSGKMGPGFTKALGHGVDLGHIYGDNLER QYQLRLFKDGKLKYQMLNGEVYPPSVEEAPVLMHYPRGIPPQSQMAVGQEVFGLLPGLML YATIWLREHNRVCDLLKAEHPTWGDEQLFQTARLILIGETIKIVIEEYVQQLSGYFLQLK FDPELLFGAQFQYRNRIAMEFNQLYHWHPLMPDSFRVGPQDYSYEQFLFNTSMLVDYGVE ALVDAFSRQPAGRIGGGRNIDHHILHVAVDVIKESRELRLQPFNEYRKRFGMKPYTSFQE LTGEKEMAAELEELYGDINALEFYLGLLLEKCHPNSIFGESMIEMGAPFSLKGLLGNPIC SPEYWKASTFGGDVGFNLVKTATLKKLVCLNTKTCPYVSFHVPDPHREDRPGVERPPTEL ...
bom:102271174 K11987 prostaglandin-endoperoxide synthase 2 [EC:1.14.99.1] , (RefSeq) PTGS2; prostaglandin-endoperoxide synthase 2 (A) MLARALLLCAAVALSGAANPCCSHPCQNRGVCMSVGFDQYKCDCTRTGFYGENCTTPEFL TRIKLLLKPTPNTVHYILTHFKGVWNIVNKISFLRNMIMRYVLTSRSHLIESPPTYNVHY SYKSWEAFSNLSYYTRALPPVPDDCPTPMGVKGRKELPDSKEVVKKVLLRRKFIPDPQGT NLMFAFFAQHFTHQFFKTDFERGPAFTKGKNHGVDLSHIYGESLERQHKLRLFKDGKMKY QMINGEMYPPTVKDTQVEMIYPPHVPEHLKFAVGQEVFGLVPGLMMYATIWLREHNRVCD VLKQEHPEWGDEQLFQTSRLILIGETIKIVIEDYVQHLSGYHFKLKFDPELLFNQQFQYQ NRIAAEFNTLYHWHPLLPDVFQIDGQEYNYQQFIYNNSVLLEHGLTQFVESFTRQRAGRV AGGRNLPVAVEKVSKASIDQSREMKYQSFNEYRKRFLLKPYESFEELTGEKEMAAELEAL YGDIDAMEFYPALLVEKPRPDAIFGETMVEAGAPFSLKGLMGNPICSPEYWKPSTFGGEV GFKIINTASIQSLICSNVKGCPFTSFSVQDTHLTKTVTINASSSHSGLDDINPTVLLKER STEL ...
Metabolism of alpha-linolenic acid and linoleic acid to their respective acids. Both of these processes are catalyzed primarily by FADS1 and FADS2. The conversion of arachidonic acid to prostanoids is catalysed by prostaglandin G/H synthase 2 and the conversion of arachidonic acid to lipoxins is catalysed by different types of lipoxygenases ...
We investigated the effects of Th2 cell-associated cytokines, IL-4, IL-10, and IL-13, on prostaglandin (PG) production by human peripheral blood monocytes (HPBM) in terms of four parameters: PGE2 synthesis; cyclooxygenase activity; protein; and mRNA of two cyclooxygenase isozymes (cyclooxygenase-1 and cyclooxygenase-2). LPS-stimulated PGE2 synthesis and cyclooxygenase activity were suppressed by IL-4, IL-10, or IL-13. Furthermore, the LPS-dependent increase of cyclooxygenase activity in HPBM was attributable to cyclooxygenase-2 because it was inhibited by NS-398 (a cyclooxygenase-2-specific inhibitor). Western and Northern blot analyses revealed that the LPS-induced increases in cyclooxygenase-2 protein and mRNA were attenuated by the addition of IL-4, IL-10, or IL-13. In contrast, cyclooxygenase-1 protein and mRNA were hardly detected in monocytes that were incubated with or without LPS in the presence or absence of IL-4, IL-10, and IL-13. These results suggest that the reduction of LPS-induced ...
PTGS2 is the inducible isozyme of prostaglandin-endoperoxide synthase, also known as cyclooxygenase. It has been linked to numerous conditions, especially involving inflammation or cancer. Also known as COX2. [PMID 17479405] Haplotypes A-1195G-765T8473 and A-1195C-765T8473 variants of COX-2 were associated with 1.3X increased risk of breast cancer in a Chinese population [PMID 16361272] Relative to individuals with a PTGS2 Ex10 +837 TT genotype, those carrying the C allele (TC or CC genotype) had a 1.8-fold risk of bile duct cancer in a Chinese population [PMID 12920574] In a group of Pima Indians, individuals with the variant PTGS2 rs20417 CC genotype had a 30% higher Type 2 diabetes prevalence compared with subjects with the GG genotype ...
Fingerprint Dive into the research topics of Reaction of aldehydes with the H,sub,5,/sub,PV,sub,2,/sub,Mo,sub,10,/sub,O,sub,40,/sub, polyoxometalate and cooxidation of alkanes with molecular oxygen. Together they form a unique fingerprint. ...
Prostaglandin G/H synthases (PGHS), commonly referred to as cyclooxygenases (COX-1 and COX-2), catalyze a key step in the synthesis of biologically active prostaglandins (PGs), the conversion of arachidonic acid (AA) into prostaglandin H2 (PGH2). PGs have important functions in a variety of physiologic and pathologic settings, including inflammation, cardiovascular homeostasis, reproduction, and carcinogenesis. However an evaluation of prostaglandin function in early mammalian development has been difficult due to the maternal contribution of prostaglandins from the uterus. The emergence of zebrafish as a model system has begun to provide some insights into the roles of this signaling cascade during vertebrate development. In zebrafish, COX-1 derived prostaglandins are required for two distinct stages of development, namely during gastrulation and segmentation. During gastrulation, PGE2 signaling promotes cell motility, without altering the cell shape or directional migration of gastrulating ...
1PGE: Synthesis and use of iodinated nonsteroidal antiinflammatory drug analogs as crystallographic probes of the prostaglandin H2 synthase cyclooxygenase active site.
Biosynthesis of TxA2 and the PG involves the sequential metabolism of AA in three stages. The first rate-limiting step is the stimulus-induced mobilization of AA from cell membrane phosphoglycerides by the enzymes phospholipase (PL) A2 (acting on phosphatidylcholine) and diacylglycerol (DAG) lipase (acting on phosphatidylinositol). The second is the oxidation of AA to the PG endoperoxides by the enzyme PG endoperoxide synthase, also known as cyclooxygenase (COX). This involves two sequential actions by the enzyme: first, the conversion of AA to endoperoxide PGG2 (COX activity), and, subsequently, the conversion of PGG2 to endoperoxide PGH2 (peroxidase activity). In the third and final stage, PGH2 is isomerized into the biologically active prostanoid end products by specific PG synthase enzymes (9, 59, 71). For TxA2 biosynthesis, this involves the action of TxA2 synthase (TxS) on PGH2 to produce TxA2. The profile of prostanoid end products produced within each tissue varies and is determined ...
The primary effect of nonsteroidal anti-inflammatory drugs (NSAIDs) is to inhibit cyclo-oxygenase (prostaglandin H synthase, or PGHS), thereby impairing the ultimate transformation of arachidonic acid to prostaglandins, prostacyclin, and thromboxanes
CONSTRUCTION AND OPTIMIZATION OF STRUCTURE-BASED VIRTUAL SCREENING PROTOCOLS TO IDENTIFY CYCLOOXYGENASE-1 INHIBITORS USING OPEN BABEL, SPORES AND PLANTS
A series of nonsteroidal anti-inflammatory drugs (NSAIDs) [S(+)-naproxen, ibuprofen isomers, and indomethacin] were evaluated for their activation of peroxisome proliferator-activated receptor (PPAR) α and γ isoforms in CV-1 cells co-transfected with rat PPAR α and γ, and peroxisome proliferator response element (PPRE)-luciferase reporter gene plasmids, for stimulation of peroxisomal fatty acyl CoA β-oxidase activity in H4IIEC3 cells, and for comparative inhibition of ovine prostaglandin endoperoxide H synthase (PGHS)-1 and PGHS-2 and arachidonic acid-induced human platelet activation. Each drug produced a concentration-dependent activation of the PPAR isoforms and fatty acid β-oxidase activity, inhibition of human arachidonic acid-induced platelet aggregation and serotonin secretion, and inhibition of PGHS-1 and PGHS-2 activities. For PPARα activation in CV-1 and H4IIEC3 cells, and the stimulation of fatty acyl oxidase activity in H4IIEC3 cells, the rank order of stereoselectivity was ...
Cyclooxygenase (COX), officially known as prostaglandin-endoperoxide synthase (PTGS), is an enzyme that is responsible for formation of important biological mediators called prostanoids, including prostaglandins, prostacyclin and thromboxane. Pharmacological inhibition of COX can provide relief from the symptoms of inflammation and pain. Drugs, like Aspirin, that inhibit cyclooxygenase activity have been available to the public for about 100 years. Two cyclooxygenase isoforms have been identified and are referred to as COX-1 and COX-2. Under many circumstances the COX-1 enzyme is produced constitutively (i.e., gastric mucosa) whereas COX-2 is inducible (i.e., sites of inflammation). Non-steroidal anti-inflammatory drugs (NSAID), such as aspirin and ibuprofen, exert their effects through inhibition of COX. The main COX inhibitors are the non-steroidal anti-inflammatory drugs (NSAIDs).. ...
The size of the PCR products from cyclooxygenase-1 and cyclooxygenase-2 are 524 and 583 base pairs, respectively. The specificity of the PCR reaction for cyclooxygenase-1 and cyclooxygenase-2 complementary deoxyribonucleic acid (cDNA) was confirmed by digestion of PCR products by sequence-specific restriction enzymes (cyclooxygenase-1: Sac I and Sma I; cyclooxygenase-2: Pst I and Nco I). For quantitation of cyclooxygenase-1 and cyclooxygenase-2 mRNA levels, the Escherichia coli plasmid pT2M containing specific internal standards for cyclooxygenase-1 and cyclooxygenase-2 was constructed by internal deletion of sequences: The truncated fragments (320 base pairs) from cyclooxygenase-1 and cyclooxygenase-2 PCR products were incorporated into the E. coli cloning plasmid pBSII SK(+)(Stratagene, La Jolla, CA) at the EcoR I and Kpn I restriction sites and multiplied as plasmids in an E. coli strain Dh5 alpha. Plasmid solutions were adjusted to 1 x 104molecules/micro liter after double digestion by ...
Non-steroidal anti-inflammatory drugs (NSAIDs), which include over-the-counter pharmaceuticals such as ibuprofen, naproxen, and aspirin, rank among the most widely used pharmaceuticals worldwide. Their chief mechanism of action is inhibition of two forms of cyclo-oxygenase (COX), namely COX-1 and COX-2 (1). Also known as prostaglandin-endoperoxide synthase (PTGS), COX is responsible for the production of downstream mediators of pain and inflammation, such as thromboxane and prostaglandins. Due to their suppression of prostaglandins, which exert protective roles in the gastrointestinal tract, one of the most frequent adverse effects of NSAIDs is irritation of the gastric mucosa.. Thus, newer generation selective COX-2 drugs, known as the coxibs, were introduced in the 1990s to mitigate the risk of peptic ulceration that results from COX-1 suppression. By 2004, coxibs had dominated the prescription drug market for NSAIDs, with worldwide sales of approximately $10 billion (2). Their development was ...
Fingerprint Dive into the research topics of In vitro investigation of the interaction between nitric oxide and cyclo-oxygenase activity in equine ventral colon smooth muscle. Together they form a unique fingerprint. ...
Ibuprofen is a well-established non-steroidal anti-inflammatory drug, inhibiting the prostaglandin-endoperoxide synthase. One of the key features defining the ibuprofen structure is the doubly intermolecular O-H⋯O [[double bond, length as m-dash]] C hydrogen bond in cyclic dimers as know from carboxylic acids a...
Cystic fibrosis (CF) is one of the most common autosomal recessive diseases among Caucasians caused by a mutation in the CFTR gene. However, the clinical outcome of CF pulmonary disease varies remarkably even in patients with the same CFTR genotype. This has led to a search for genetic modifiers located outside the CFTR gene. The aim of this study was to evaluate the effect of functional variants in prostaglandin-endoperoxide synthase genes (COX1 and COX2) on the severity of lung disease in CF patients. To the best of our knowledge, it is the first time when analysis of COX1 and COX2 as potential CF modifiers is provided. The study included 94 CF patients homozygous for F508del mutation of CFTR. To compare their clinical condition, several parameters were recorded, e.g. a unique clinical score: disease severity status (DSS). To analyse the effect of non-CFTR genetic polymorphisms on the clinical course of CF patients, the whole coding region of COX1 and selected COX2 polymorphisms were analysed. ...
Purified Terephthalic Acid Market: By Manufacturing Process (Amoco Process, Cooxidation, Multistage Oxidation, Henkel Process), By Application (Polyester Production, Cyclohexanedimethanol Production, Others) & By Region-Forecast (2016-2021) - Market research report and industry analysis - 10581722
Resistance to immunotherapy is one of the biggest problems of current oncotherapeutics. While T cell abundance is essential for tumor responsiveness to immunotherapy, factors that define the T cell-inflamed tumor microenvironment are not fully understood. We used an unbiased approach to identify tumor-intrinsic mechanisms shaping the immune tumor microenvironment (TME), focusing on pancreatic adenocarcinoma because it is refractory to immunotherapy and excludes T cells from the TME. From human tumors, we identified ephrin-A receptor 2 (EPHA2) as a candidate tumor-intrinsic driver of immunosuppression. Epha2 deletion reversed T cell exclusion and sensitized tumors to immunotherapy. We found that prostaglandin endoperoxide synthase 2 (PTGS2), the gene encoding cyclooxygenase-2, lies downstream of EPHA2 signaling through TGF-β and is associated with poor patient survival. Ptgs2 deletion reversed T cell exclusion and sensitized tumors to immunotherapy; pharmacological inhibition of PTGS2 was ...
Title:Inflammatory Cyclooxygenase Activity and PGE,sub,2,/sub, Signaling in Models of Alzheimers Disease. VOLUME: 11 ISSUE: 2. Author(s):Jenny U. Johansson, Nathaniel S. Woodling, Ju Shi and Katrin I. Andreasson. Affiliation:Stanford University School of Medicine, 1201 Welch Road, Stanford, CA 94305, USA.. Keywords:Alzheimers disease, microglia, amyloid beta, inflammation, cyclooxgenases, prostaglandin E2, EP2 receptor, EP3 receptor, EP4 receptor.. Abstract:The inflammatory response is a fundamental driving force in the pathogenesis of Alzheimers disease (AD). In the setting of accumulating immunogenic Aß peptide assemblies, microglia, the innate immune cells of the brain, generate a non-resolving immune response and fail to adequately clear accumulating Aß peptides, accelerating neuronal and synaptic injury. Pathological, biomarker, and imaging studies point to a prominent role of the innate immune response in AD development, and the molecular components of this response are beginning to ...
Cyclooxygenase is the key enzyme in the biosynthetic pathway of prostaglandins (PGs) and thromboxane from arachidonic acid. There are two isozymes of cyclooxygenase; constitutive cyclooxygenase-1 and...
Weggen S, Eriksen JL, Das P, Sagi SA, Wang R, Pietrzik CU, Findlay KA, Smith TE, Murphy MP, Bulter T, Kang DE, Marquez-Sterling N, Golde TE, Koo EH. A subset of NSAIDs lower amyloidogenic Abeta42 independently of cyclooxygenase activity ...
Epidemiological and clinical studies suggest that non-steroidal anti-inflammatory drugs (NSAIDs), including cyclooxygenase (COX)-2 selective inhibitors, reduce the risk of developing cancer. Experimental studies in human cancer cell lines and rodent models of carcinogenesis support these observations by providing strong evidence for the antineoplastic properties of NSAIDs. The involvement of COX-2 in tumorigenesis and its overexpression in various cancer tissues suggest that inhibition of COX-2 is responsible for the chemopreventive efficacy of these agents. However, the precise mechanisms by which NSAIDs exert their antiproliferative effects are still a matter of debate. Numerous other studies have shown that NSAIDs can act through COX-independent mechanisms. This review provides a detailed description of the major COX-independent molecular targets of NSAIDs and discusses how these targets may be involved in their anticancer effects. Toxicities resulting from COX inhibition and the suppression of
We thank Drs. Gasparovic and Petricevic for their interest in our study (1) and their comments. They strongly suggest that P2Y12-based platelet function assays should be complemented with cyclooxygenase-dependent testing in framing the therapeutic windows for dual antiplatelet therapy. We think that this statement is highly speculative and not supported by the available evidence. Indeed, aspirin resistance has been extensively discussed as a real entity by itself and its association with clinical outcomes. First, response to aspirin assessed by cyclooxygenase-dependent testing has probably been overestimated due to a problem of compliance, and a previous study by our group showed that noncompliance was the main explanation for aspirin resistance, being a rare entity in compliant patients (2). For ischemic risk, some studies suggest the potential impact of aspirin resistance on ischemic events (3), but a recent study assessing the benefit of tailored therapy based on platelet testing of aspirin ...
Background Giardia lamblia trophozoites colonize in the upper small intestine resulting in diarrhea and various clinical manifestations, including abdominal pain, anorexia, and signs of malabsorption. A decrease in the level of trace elements might occur because of this absorption deficiency resulting from giardiasis. Experimentally, the excretory secretory product of G. lamblia trophozoites increased the level of reactive oxygen species in mice enterocytes. The levels of bilirubin, uric acid, and albumin are often used as major nonenzymatic oxidative biomarkers. Objective This study was designed to determine the effect of therapy by metronidazole (MTZ) and artemether (ART) on trophozoite and cyst forms in experimentally Giardia spp.-infected hamsters and to reveal the changes in iron (Fe), manganese (Mn), copper (Cu), and chromium (Cr) serum levels pretreatment and post-treatment. Another objective was to evaluate the impact of this therapy on serum levels of bilirubin, uric acid, and albumin ...
COX-2 Drugs were recently approved by FDA, USA. After the discovery of COX-2, several new medicines were produced and unlike the earlier NSAIDs, the side effects were significantly reduced. COX-2 medicines were proved to be safer than COX-1 medicines. Even the doctors are prescribing these COX-2 medicines only because of their advantages over COX-1 medicines.. There is a clear difference in DNA and mRNA structures of these two but the end results are same. Even the structure of these two enzymes is almost 60% similar. The effects of these enzymes on arachidonic acid are almost same but their functionality is different. COX-2 is localized to nuclear membrane and endoplasmic reticulum. COX-1 is localized to later one only. For prostaglandin synthesis, these two use different versions of arachidonate.. The best thing about COX-2 is it doesn’t affect the prostaglandins that cause these GI problems in any way. It just stops the synthesis and the user won’t face any discomforts like GI ...
Prostaglandins and glucocorticoids are potent mediators of inflammation. Non-steroidal anti-inflammatory drugs (NSAIDs) exert their effects by inhibition of prostaglandin production. The pharmacological target of NSAIDs is cyclooxygenase (COX, also known as PGH synthase), which catalyses the first committed step in arachidonic-acid metabolism. Two isoforms of the membrane protein COX are known: COX-1, which is constitutively expressed in most tissues, is responsible for the physiological production of prostaglandins; and COX-2, which is induced by cytokines, mitogens and endotoxins in inflammatory cells, is responsible for the elevated production of prostaglandins during inflammation. The structure of ovine COX-1 complexed with several NSAIDs has been determined. Here we report the structures of unliganded murine COX-2 and complexes with flurbiprofen, indomethacin and SC-558, a selective COX-2 inhibitor, determined at 3.0 to 2.5 A resolution. These structures explain the structural basis for the ...
Sevigny M.B., Li C.F., Alas M., Hughes-Fulford M.. Cyclooxygenase-2 (COX-2) catalyzes the rate-limiting step in the prostanoid biosynthesis pathway, converting arachidonic acid into prostaglandin H(2). COX-2 exists as 72 and 74kDa glycoforms, the latter resulting from an additional oligosaccharide chain at residue Asn(580). In this study, Asn(580) was mutated to determine the biological significance of this variable glycosylation. COS-1 cells transfected with the mutant gene were unable to express the 74kDa glycoform and were found to accumulate more COX-2 protein and have five times greater COX-2 activity than cells expressing both glycoforms. Thus, COX-2 turnover appears to depend upon glycosylation of the 72kDa glycoform.. FEBS Lett. 580:6533-6536(2006) [PubMed] [Europe PMC] ...
The active ingredient in aspirin is acetylsalicyacetic acid (ASA). It works by chemically modifying an enzyme which is responsible, in part, for causing fever and inflammation. The enzyme is known by several names in the scientific literature, including: cyclooxygenase (COX), prostaglandin synthase (PGS). It turns out that there are two closely related forms of this enzyme, so they are now numbered: COX-1 and COX-2 or PGS-1 and PGS-2. The acetyl group in ASA reacts with a permanently binds to the active site of these enzymes, such that they no longer work. However, over a period of several hours, most cells make new enzyme which does work. That is why you have to keep taking aspirin for the effect to last. So I have not really explained how these two related enzymes cause fever and inflammation. Well it turns out that the second form of the enzyme (i.e., COX-2 or PGS-2), is turned on during an infection or injury. This enzyme is responsible for the generation of compounds known as prostaglandins ...
The role of prostaglandin H synthase (PHS) in the metabolism of 7,8-dihydroxy-7,8-dihydrobenzo[a]pyrene (BP-7,8-diol) has been… Expand ...
Ibuprofen has analgesic, anti-inflammatory and antipyretic action due to inhibition of biosynthesis of prostaglandins by inhibiting the enzyme cyclooxygenase.
two can be acting not solely via cAMP but additionally through PLC, which is usually a downstream effector of EP3 receptors (Asboth et al. 1996); PLC inhibition substantially decreased the response to PGE2 . PGE2 stimulates HA production in lots of other tissues too, such as atheroma (Marzoll et al. 2009). Moreover, synovium express the important synthetic enzymes COX1 and COX2 (Satoh et al. 2008). Nevertheless, PGE2 did not seem to mediate MSHA, since neither the common COX inhibitor indomethacin nor a combination ofC2009 The Authors. Journal compilationC2009 The Physiological SocietyJ Physiol 587.Pathways regulating movement-stimulated Altered functional expression of TRPV1168. To evaluate this possibility, we examined hyaluronan secretionspecific COX1 and COX2 inhibitors inhibited MSHA (Table four, study six). PGE2 In the mutants and also the genetically rescued worms in the WSA levels are raised in arthritis, where their pronounced HA-stimulating effect is probably to be vital in helping ...
Liu, X., Wong, P.T.-H., Lee, T.L. (2006). Cyclooxygenase-1 inhibition shortens the duration of diazepam-induced loss of righting reflex in mice. Anesthesia and Analgesia 102 (1) : 135-140. [email protected] Repository. https://doi.org/10.1213/01.ane.0000189102.09347. ...
PTGIS - PTGIS (untagged)-Human prostaglandin I2 (prostacyclin) synthase (PTGIS) available for purchase from OriGene - Your Gene Company.
Wendeburg, L., de Oliveira, A.C., Bhatia, H.S., Candelario-Jalil, E. and Fiebich, B.L. (2009) Resveratrol inhibits prostaglandin formation in IL-1beta-stimulated SK-NSH neuronal cells. Journal of Neuroinflammation, 14, 26.
... (prostaglandin G/H synthase and cyclooxygenase) (The HUGO official symbol is PTGS2; HGNC ... prostaglandin-endoperoxide synthase activity. Cellular component. • cytoplasm. • endoplasmic reticulum lumen. • membrane. • ... Smith WL, Garavito RM, DeWitt DL (December 1996). "Prostaglandin endoperoxide H synthases (cyclooxygenases)-1 and -2". J. Biol ... PTGS2, COX-2, COX2, GRIPGHS, PGG/HS, PGHS-2, PHS-2, hCox-2, prostaglandin-endoperoxide synthase 2. ...
An exception to this is the prostaglandin-endoperoxide synthase. The EGF-like domain includes 6 cysteine residues which in the ...
The names "prostaglandin synthase (PHS)", "prostaglandin synthetase (PHS)", and "prostaglandin-endoperoxide synthetase (PES)" ... Liu J, Seibold SA, Rieke CJ, Song I, Cukier RI, Smith WL (June 2007). "Prostaglandin endoperoxide H synthases: peroxidase ... Cyclooxygenase (COX), officially known as prostaglandin-endoperoxide synthase (PTGS), is an enzyme (specifically, a family of ... A member of the animal-type heme peroxidase family, it is also known as prostaglandin G/H synthase. The specific reaction ...
"The membrane binding domains of prostaglandin endoperoxide H synthases 1 and 2. Peptide mapping and mutational analysis". J ...
"The membrane binding domains of prostaglandin endoperoxide H synthases 1 and 2. Peptide mapping and mutational analysis". ...
Tissues with low CYP-450 expression use the prostaglandin endoperoxide synthase (PES) instead. This oxidative pathway ... Lang, B.; Frei, K.; Maier, P. (1986-10-15). "Prostaglandin synthase dependent aldrin epoxidation in hepatic and extrahepatic ... bisdioxygenises the arachidonic acid to prostaglandin G2 (PGG2). Subsequently, PGG2 is reduced to prostaglandin H2 (PGH2) by ...
... officially known as prostaglandin-endoperoxide synthase, PTGS) enzyme required for prostaglandin and thromboxane synthesis. ... Aspirin-modified PTGS2 (Prostaglandin-endoperoxide synthase 2) produces lipoxins, most of which are anti-inflammatory.[ ... Prostaglandins, local hormones produced in the body, have diverse effects, including the transmission of pain information to ... Like its ability to control pain, aspirin's ability to control fever is due to its action on the prostaglandin system through ...
... also known as prostaglandin G/H synthase 1, prostaglandin-endoperoxide synthase 1 or prostaglandin H2 synthase 1, is an enzyme ... "Entrez Gene: PTGS1 prostaglandin-endoperoxide synthase 1 (prostaglandin G/H synthase and cyclooxygenase)". Chandrasekharan NV, ... Prostaglandin-endoperoxide synthase (PTGS), also known as cyclooxygenase (COX), is the key enzyme in prostaglandin biosynthesis ... Otto JC, DeWitt DL, Smith WL (August 1993). "N-glycosylation of prostaglandin endoperoxide synthases-1 and -2 and their ...
"Fatty acid substrate specificities of human prostaglandin-endoperoxide H synthase-1 and -2. Formation of 12-hydroxy-(9Z, 13E/Z ... "Prostaglandin H-Synthase-2 is the Main Enzyme Involved in the Biosynthesis of Octadecanoids from Linoleic Acid in Human Dermal ... Prostaglandins & Other Lipid Mediators. 81 (1-2): 1-13. doi:10.1016/j.prostaglandins.2006.05.024. PMID 16997127. Kelavkar, U. P ... doi:10.1016/j.prostaglandins.2008.11.002. PMID 19063986. Yin, Hong; Chu, Alan; Li, Wei; Wang, Bin; Shelton, Fabiola; Otero, ...
... stimulates prostaglandin E2 production by activating COX-1 and prostaglandin endoperoxide synthase-1 but inhibites ... Additionally, expression of the prostaglandin E2 receptor, the most upregulated target gene in the β-catenin pathway of DP ... ". "HMGB1 promotes hair growth via the modulation of prostaglandin metabolism". Suchonwanit P, Thammarucha S, Leerunyakul K ( ...
This gene represents transcription of a long non-coding RNA produced in antisense to the prostaglandin-endoperoxide synthase 2 ...
... expression of prostaglandin-endoperoxide synthase 2 by somatic and spermatogenic cells is responsible for prostaglandin E2 ... Examples are prostaglandin E2, inducible nitric oxide synthase (iNOS), TNFα and IL-1β, although at lower levels than other ... Bauché F, Stéphan JP, Touzalin AM, Jégou B (1995). "In vitro regulation of an inducible-type NO synthase in the rat ... O'Bryan MK, Schlatt S, Gerdprasert O, Phillips DJ, de Kretser DM, Hedger MP (2000). "Inducible nitric oxide synthase in the rat ...
"Fatty acid substrate specificities of human prostaglandin-endoperoxide H synthase-1 and -2. Formation of 12-hydroxy-(9Z, 13E/Z ... "Prostaglandins & Other Lipid Mediators. 104-105: 139-43. doi:10.1016/j.prostaglandins.2012.08.004. PMC 3532570. PMID 22960430. ... "Prostaglandin H-Synthase-2 is the Main Enzyme Involved in the Biosynthesis of Octadecanoids from Linoleic Acid in Human Dermal ... Prostaglandins & Other Lipid Mediators. 81 (1-2): 1-13. doi:10.1016/j.prostaglandins.2006.05.024. PMID 16997127.. ...
11-Eicosatrienoic Acid by Prostaglandin Endoperoxide Synthase and by Cytochrome P450 Monooxygenase: Structure and Mechanism of ... "PROSTAGLANDINS AND RELATED COMPOUNDS". Archived from the original on April 13, 2018. Retrieved October 24, 2007. EN Siguel; KM ... Cyclooxygenase breaks the bisallylic C-H bond of AA to synthesize prostaglandin H2, but breaks a stronger allylic C-H bond when ... Eicosanoid Prostaglandin Siegel, George J.; Albers, R. Wayne (2006). Basic neurochemistry: molecular, cellular, and medical ...
... officially known as prostaglandin-endoperoxide synthase, PTGS) enzyme required for prostaglandin and thromboxane synthesis. ... Prostaglandins and thromboxanes[edit]. Aspirin's ability to suppress the production of prostaglandins and thromboxanes is due ... Like its ability to control pain, aspirin's ability to control fever is due to its action on the prostaglandin system through ... Prostaglandins, local hormones produced in the body, have diverse effects, including the transmission of pain information to ...
Smith, W. L.; Song, I (2002). "The enzymology of prostaglandin endoperoxide H synthases-1 and -2". Prostaglandins & other lipid ... prostaglandin G/H synthase 1 and 2 {PTGS1 and PTGS2}) metabolize arachidonic acid to prostaglandin G2 and prostaglandin H2, ... Wlodawer, P; Samuelsson, B (1973). "On the organization and mechanism of prostaglandin synthetase". The Journal of Biological ... Arachidonic acid promotes the repair and growth of skeletal muscle tissue via conversion to prostaglandin PGF2alpha during and ...
... prostaglandin-endoperoxide synthase) and lipoxygenases (LOX) (also known as: EC 1.13.11.34, EC 1.13.11.33, etc.). ... Many of these prostaglandins are inflammatory and vasoconstrictive. Prostaglandins are signalled through two varying pathways ... trenbolone acetate's androgenic effect activates a variety of lipid-like active compounds which are called prostaglandins. ...
... cells that express constitutive prostaglandin-endoperoxide H synthase-2. Basis for low protaglandin E2 production". J. Biol. ... Microsomal prostaglandin E synthase-1 (mPGES-1) or Prostaglandin E synthase is an enzyme that in humans is encoded by the PTGES ... 2002). "Expression of prostaglandin I(2) synthase, but not prostaglandin E synthase, changes in myometrium of women at term ... 2003). "Cellular prostaglandin E2 production by membrane-bound prostaglandin E synthase-2 via both cyclooxygenases-1 and -2". J ...
Proc Natl Acad Sci 91:5252-5256, 1994 Marcheselli VL, Bazan NG: Sustained induction of prostaglandin endoperoxide synthase-2 by ... Moreover, they found that PAF activates transcription of the inducible prostaglandin synthase, cyclooxygenase-2 (COX-2). ... Prostaglandins 27:203-216, 1984 Birkle DL, Bazan NG: Effects of K+ depolarization on the synthesis of prostaglandins and ... Lipocalin-type prostaglandin D synthase (β-trace) is located in pigment epithelial cells of rat retina and accumulates within ...
... polyketide synthases MeSH D08.811.600.720 - prostaglandin-endoperoxide synthases MeSH D08.811.600.720.500 - cyclooxygenase 1 ... prostaglandin-endoperoxide synthases MeSH D08.811.682.690.708.749 - squalene monooxygenase MeSH D08.811.682.690.708.783 - ... riboflavin synthase MeSH D08.811.913.225.825 - spermidine synthase MeSH D08.811.913.225.912 - spermine synthase MeSH D08.811. ... nitric oxide synthase type i MeSH D08.811.682.664.500.772.500 - nitric oxide synthase type ii MeSH D08.811.682.664.500.772.750 ...
... also termed prostaglandin-endoperoxide synthase-1 (PTGS1) and PTGS2, respectively) metabolize arachidonic acid by adding ... PGF synthase which converts PGH2 to PGF2α; c) Prostaglandin D2 synthase which converts PGH2 to PGD2 (subsequent products in ... It is metabolized by (see diagram in Prostanoids: a) the Prostaglandin E synthase pathway in which any one of three isozymes, ... doi:10.1016/j.prostaglandins.2011.09.001. PMID 21945326. Matsuoka T, Narumiya S (2007). "Prostaglandin receptor signaling in ...
"The membrane binding domains of prostaglandin endoperoxide H synthases 1 and 2. Peptide mapping and mutational analysis". J ...
Cells can use prostaglandin-endoperoxide synthase 1 (i.e. cyclooxygenenase-1 or COX-1) and Prostaglandin-endoperoxide synthase ... HETE by ubiquitous cellular peroxidase reactions including those possessed by prostaglandin-endoperoxide synthase-1 and -2, ... "Prostaglandin H synthase: Distinct binding sites for cyclooxygenase and peroxidase substrates". Archives of Biochemistry and ... Prostaglandins & Other Lipid Mediators. 89 (3-4): 120-5. doi:10.1016/j.prostaglandins.2008.12.003. PMID 19130894. Sachs-Olsen, ...
Christ-Hazelhof E, Nugteren DH (1979). "Purification and characterisation of prostaglandin endoperoxide D-isomerase, a ... Prostaglandin D2 synthase Hematopoietic prostaglandin D synthase Garza, L. A.; Liu, Y.; Yang, Z.; Alagesan, B.; Lawson, J. A.; ... Other names in common use include prostaglandin-H2 Delta-isomerase, prostaglandin-R-prostaglandin D isomerase, and PGH-PGD ... In enzymology, a prostaglandin-D synthase (EC 5.3.99.2) is an enzyme that catalyzes the chemical reaction (5Z,13E)-(15S)-9alpha ...
... (prostaglandin G/H synthase and cyclooxygenase) (The HUGO official symbol is PTGS2; HGNC ... "Prostaglandin endoperoxide H synthases (cyclooxygenases)-1 and -2". J. Biol. Chem. 271 (52): 33157-60. doi:10.1074/jbc.271.52. ... Furthermore, the product of PTGS2 (COX-2), PGH2 is converted by prostaglandin E2 synthase into PGE2, which in turn can ... Dean AM, Dean FM (May 1999). "Carbocations in the synthesis of prostaglandins by the cyclooxygenase of PGH synthase? A radical ...
PGE2 to bind to its receptor as oppose to generally blocking viable receptors such as prostaglandin endoperoxide synthase or ... A prostaglandin antagonist is a hormone antagonist acting upon one or more prostaglandins, a subclass of eicosanoid compounds ... Prostaglandin antagonists may also help with allergies, primarily seasonal allergies or nasal allergies. The prostaglandin D2 ( ... NSAIDs are perhaps the best-known prostaglandin antagonists; they suppress the signaling function of prostaglandins, which are ...
Prostaglandin-endoperoxide synthase 1 (en) eta Prostaglandin-endoperoxide synthase 2 (en) Hartzeko bidea. aho bidez. ... Antiinflamatorio ez esteroideo, prostaglandin antagonist (en) , antipiretiko, cyclooxygenase inhibitor (en) eta fibrinolytic ...
Smith W. L., Song I (2002)։ «The enzymology of prostaglandin endoperoxide H synthases-1 and -2»։ Prostaglandins & other lipid ... 22,0 22,1 «Effects of prostaglandins and COX-inhibiting drugs on skeletal muscle adaptations to exercise»։ J. Appl. Physiol. ... Wlodawer P, Samuelsson B (1973)։ «On the organization and mechanism of prostaglandin synthetase»։ The Journal of Biological ...
Smith, W. L.; Song, I (2002). "The enzymology of prostaglandin endoperoxide H synthases-1 and -2". 《Prostaglandins & other ... Wlodawer, P; Samuelsson, B (1973). "On the organization and mechanism of prostaglandin synthetase". 《The Journal of Biological ... "Effects of prostaglandins and COX-inhibiting drugs on skeletal muscle adaptations to exercise". 《J. Appl. Physiol.》 115 (6): ...
Wang LH, Kulmacz RJ (2002). "Thromboxane synthase: structure and function of protein and gene". Prostaglandins and Other Lipid ... In the first step of the mechanism, the heme iron coordinates to the C-9 endoperoxide oxygen. It participates in homolytic ... Wang LH, Kulmacz RJ (2003). "Thromboxane synthase: structure and function of protein and gene". Prostaglandins Other Lipid ... Cathcart MC; Reynolds JV; O'Byrne KJ; Pidgeon GP (2010). "The role of prostacyclin synthase and thromboxane synthase signaling ...
"The membrane binding domains of prostaglandin endoperoxide H synthases 1 and 2. Peptide mapping and mutational analysis". J ...
Gelosa P, Sevin G, Pignieri A, Budelli S, et al «Terutroban, a thromboxane/prostaglandin endoperoxide receptor antagonist, ... Davı, G; Santilli, F; Vazzana, N «Thromboxane Receptors Antagonists and/or Synthase Inhibitors» (en anglès). A: Antiplatelet ...
"Prostaglandin endoperoxides. Novel transformations of arachidonic acid in human platelets". Proceedings of the National Academy ... prostaglandin H2 (PGH2). Thromboxane synthase further metabolizes PGH2 to the 20 carbon product, Thromboxane A2, the 17 carbon ... Prostaglandin E2 and Prostaglandin D2, but not 12 other lipoxygenase or cycloxygenase mebolites showed a statistically ... "Xenobiotic-metabolizing cytochromes P450 convert prostaglandin endoperoxide to hydroxyheptadecatrienoic acid and the mutagen, ...
The series-3 prostaglandin PGH3 also follows the prostacyclin synthase pathway, yielding another prostacyclin, PGI3.[12] The ... "An enzyme isolated from arteries transforms prostaglandin endoperoxides to an unstable substance that inhibits platelet ... Prostacyclin (also called prostaglandin I2 or PGI2) is a prostaglandin member of the eicosanoid family of lipid molecules. It ... prostaglandin I1, and prostaglandin I3". Journal of the American Chemical Society. 100 (24): 7690. doi:10.1021/ja00492a043.. ...
Ohki S, Ogino N, Yamamoto S, Hayaishi O (1979). "Prostaglandin hydroperoxidase, an integral part of prostaglandin endoperoxide ... Harvison PJ, Egan RW, Gale PH, Nelson SD (1986). "Acetaminophen as a cosubstrate and inhibitor of prostaglandin H synthase". ... Its clinical pharmacologic characteristics reflect its inhibition of the two prostaglandin H2 synthases". Clin. Pharmacol. Ther ...
5-Hydroxyeicosatetraenoic acid 15-Hydroxyeicosatetraenoic acid Hamberg, M; Samuelsson, B (1974). "Prostaglandin endoperoxides. ... a product made when prostaglandin H2 is metablized to Thromboxane A2 by Thromboxane synthase or spontaneously rearranges non- ... In other tissues and animal species, numerous hepoxilins form but the hepoxilin synthase activity responsible for their ... Yoshimoto, T; Takahashi, Y (2002). "Arachidonate 12-lipoxygenases". Prostaglandins & other lipid mediators. 68-69: 245-62. doi: ...
... prostaglandin-endoperoxide synthase) and lipoxygenases (LOX) (also known as: EC 1.13.11.34, EC 1.13.11.33, etc.).[22] ... Many of these prostaglandins are inflammatory and vasoconstrictive. Prostaglandins are signalled through two varying pathways ... trenbolone acetate's androgenic effect activates a variety of lipid-like active compounds which are called prostaglandins[ ...
Nonenzymatic production of prostaglandin endoperoxides during autoxidation". J. Org. Chem. 40 (24): 3615-7. doi:10.1021/ ... This product is further metabolized by thromboxane synthase to thromboxane A2, 12-hydroxyheptadecatrienoic acid, and ... USA 71:3400; 1974 Prostaglandins Other Lipid Mediat. 1998 Jun;56(2-3):53-76 Pryor WA, Stanley JP (1975). "Letter: A suggested ... product in thromboxane A2 synthesis wherein cyclooxygenase 1 or cycloxygenase 2 metabolizes arachidonic acid to prostaglandin ...
Prostaglandin D2 synthase to create prostaglandin D2 Prostaglandin E synthase to create prostaglandin E2 It rearranges non- ... "Prostaglandin endoperoxides. 14. Solvent-induced fragmentation of prostaglandin endoperoxides. New aldehyde products from PGH2 ... Prostaglandin H2 is a type of prostaglandin and a precursor for many other biologically significant molecules. It is ... It is acted upon by: Prostacyclin synthase to create prostacyclin Thromboxane-A synthase to create thromboxane A2 and 12-(S)- ...
... and microsomal PGE synthase-1 in seminal vesicles and vas deferens". Prostaglandins & Other Lipid Mediators. 75 (1-4): 47-64. ... "Identification of CYP4F8 in human seminal vesicles as a prominent 19-hydroxylase of prostaglandin endoperoxides". The Journal ... CYP4F8 has little activity in omega-hydroxylating leukotriene B4, prostaglandin D2, prostaglandin E2, prostaglandin E1, or ... Oliw EH, Stark K, Bylund J (August 2001). "Oxidation of prostaglandin H(2) and prostaglandin H(2) analogues by human ...
... encodes a novel prostaglandin synthase/cyclooxygenase homologue". J. Biol. Chem. 266 (20): 12866-72. PMID 1712772. Kurumbail RG ... prostaglandin endoperoxides, thromboxanes, and leukotrienes. Nobel Lecture, 8 December 1982". Biosci. Rep. 3 (9): 791-813. doi: ... "Expression of a mitogen-responsive gene encoding prostaglandin synthase is regulated by mRNA splicing". Proc. Natl. Acad. Sci. ... "Determinants of the cellular specificity of acetaminophen as an inhibitor of prostaglandin H(2) synthases". Proc. Natl. Acad. ...
Prostaglandin-endoperoxide synthase 2 (prostaglandin G/H synthase and cyclooxygenase) (The HUGO official symbol is PTGS2; HGNC ... prostaglandin-endoperoxide synthase activity. Cellular component. • cytoplasm. • endoplasmic reticulum lumen. • membrane. • ... Smith WL, Garavito RM, DeWitt DL (December 1996). "Prostaglandin endoperoxide H synthases (cyclooxygenases)-1 and -2". J. Biol ... PTGS2, COX-2, COX2, GRIPGHS, PGG/HS, PGHS-2, PHS-2, hCox-2, prostaglandin-endoperoxide synthase 2. ...
Prostaglandin-endoperoxide synthase 2 (prostaglandin G/H synthase and cyclooxygenase) (The HUGO official symbol is PTGS2; HGNC ... "Prostaglandin endoperoxide H synthases (cyclooxygenases)-1 and -2". J. Biol. Chem. 271 (52): 33157-60. doi:10.1074/jbc.271.52. ... Furthermore, the product of PTGS2 (COX-2), PGH2 is converted by prostaglandin E2 synthase into PGE2, which in turn can ... Dean AM, Dean FM (May 1999). "Carbocations in the synthesis of prostaglandins by the cyclooxygenase of PGH synthase? A radical ...
prostaglandin H2 synthase 2. prostaglandin-endoperoxide synthase 2 (prostaglandin G/H synthase and cyclooxygenase). NP_000954.1 ... PTGS2 prostaglandin-endoperoxide synthase 2 [Homo sapiens] PTGS2 prostaglandin-endoperoxide synthase 2 [Homo sapiens]. Gene ID: ... prostaglandin_endoperoxide_synthase; Animal prostaglandin endoperoxide synthase and related bacterial proteins. cd00054. ... of HIV-1 gp41 upregulates the expression of prostaglandin-endoperoxide synthase 2 (PTGS2; prostaglandin G/H synthase and ...
Enzyme complexes that catalyze the formation of PROSTAGLANDINS from the appropriate unsaturated FATTY ACIDS, molecular OXYGEN, ... Prostaglandin Endoperoxide Synthases; Prostaglandin G H Synthase; Synthase, PGH; Synthase, Prostaglandin; Synthase, ... Prostaglandin G-H; Synthase, Prostaglandin H; Synthase, Prostaglandin-Endoperoxide; Synthases, Prostaglandin-Endoperoxide; ... Prostaglandin-Endoperoxide Synthases (Cyclooxygenase). Subscribe to New Research on Prostaglandin-Endoperoxide Synthases ...
Prostaglandin endoperoxide synthase 2, also referred to as cyclooxygenase 2 (COX-2), is a key enzyme in the conversion of ... Alterations in cellular adhesion and apoptosis in epithelial cells overexpressing prostaglandin endoperoxide synthase 2.. ... arachidonic acid to prostaglandins and other eicosanoids. Rat intestinal epithelial (RIE) cells were permanently transfected ...
Prostaglandin-endoperoxide synthase (PTGS1 and PTGS2) expression and prostaglandin production by normal monkey ovarian surface ... NSAIDs reduce prostaglandin production by blocking prostaglandin-endoperoxide synthase 2 (PTGS2, commonly known as COX-2), an ... Prostaglandin-endoperoxide synthase 2 (PTGS2) gene polymorphisms and risk of biliary tract cancer and gallstones: a population- ... MAIN OUTCOME MEASURE(S): Ovarian surface epithelium expression of prostaglandin-endoperoxide synthase 1 (PTGS1) and PTGS2 ...
1 from sheep has been used as positive control protein in western blot analysis of osteoarthritis samples and in prostaglandin ... Synonym: COX-1, Constitutive cyclooxygenase, Prostaglandin H synthase 1, Prostaglandin endoperoxide synthase ... COX-1 catalyzes the conversion of arachidonic acid to prostaglandin H2 (the first step in the biosynthesis of prostaglandins, ... has been used as positive control protein in western blot analysis of osteoarthritis samples and in prostaglandin synthase ...
... prostaglandin G/H synthase and cyclooxygenase)), Authors: Panagiotis A Konstantinopoulos, Michalis V Karamouzis, Athanasios G ... PTGS2 (prostaglandin-endoperoxide synthase 2 (prostaglandin G/H synthase and cyclooxygenase)). Written. 2007-05. Panagiotis A ... PTGS2 (prostaglandin-endoperoxide synthase 2 (prostaglandin G/H synthase, cyclooxygenase)). Atlas Genet Cytogenet Oncol ... a cyclooxygenase (COX) that converts arachidonic acid to a prostaglandin endoperoxide, prostaglandin G2 (PGG2), and *a ...
prostaglandin endoperoxide H synthase. PMNL. polymorphonuclear leukocyte. RIA. radioimmunoassay. TXB2. thromboxane B2 SDS-PAGE ... Potencies of Leflunomide and HR325 as Inhibitors of Prostaglandin Endoperoxide H Synthase-1 and -2: Comparison with ... Potencies of Leflunomide and HR325 as Inhibitors of Prostaglandin Endoperoxide H Synthase-1 and -2: Comparison with ... Potencies of Leflunomide and HR325 as Inhibitors of Prostaglandin Endoperoxide H Synthase-1 and -2: Comparison with ...
Prostaglandin G/H Synthase and Cyclooxygenase) (PTGS1) (AA 536-886) antibody ABIN784005 from antibodies-online ... Itemanti-Prostaglandin-Endoperoxide Synthase 1 (Prostaglandin G/H Synthase and Cyclooxygenase) (PTGS1) (AA 536-886) antibody ... anti-Prostaglandin-Endoperoxide Synthase 1 (Prostaglandin G/H Synthase and Cyclooxygenase) (PTGS1) (AA 536-886) antibody from ...
Download PDF Prostaglandin endoperoxide synthase 2 (PTGS2) and prostaglandins F2α and E2 synthases (PGFS and PGES) expression ... Prostaglandin endoperoxide synthase 2 (PTGS2) and prostaglandins F2α and E2 synthases (PGFS and PGES) expression and ... Prostaglandin endoperoxide synthase 2 (PTGS2) and prostaglandins F2α and E2 synthases (PGFS and PGES) expression and ... PG-endoperoxide synthase (PTGS2), PGF(2α) synthase (PGFS) and PGE(2) synthase (PGES). Feline endometria (n = 16) were collected ...
Polymorphisms of prostaglandin-endoperoxide synthase 2 gene, and prostaglandin-E receptor 2 gene, C-reactive protein ... Recent data have shown an association between polymorphisms of prostaglandin-endoperoxide synthase-2 gene (PTGS2; alias COX-2 ... Although these prospective data implicate the potential involvement of prostaglandin-E receptor-2 gene variation in ... and prostaglandin-E receptor-2 gene (PTGER2) and risk of atherothrombotic disorders. ...
Differential effects of thromboxane A2 synthase inhibition, singly or combined with thromboxane A2/prostaglandin endoperoxide ... Differential effects of thromboxane A2 synthase inhibition, singly or combined with thromboxane A2/prostaglandin endoperoxide ... Differential effects of thromboxane A2 synthase inhibition, singly or combined with thromboxane A2/prostaglandin endoperoxide ... Differential effects of thromboxane A2 synthase inhibition, singly or combined with thromboxane A2/prostaglandin endoperoxide ...
... for the conversion of arachidonic acid to prostaglandins in response to inflammation is prostaglandin endoperoxide synthase 2/ ... Prostaglandins are integral components in the cellular response to inflammation, promoting cellular proliferation and ... A polymorphism in the 3 untranslated region of the gene encoding prostaglandin endoperoxide synthase 2 is not associated with ... CI, confidence interval; NHS, Nurses Health Study; OR, odds ratio; PTGS2, prostaglandin endoperoxide synthase 2; WHS, Harvard ...
... prostaglandin endoperoxide synthase explanation free. What is prostaglandin endoperoxide synthase? Meaning of prostaglandin ... endoperoxide synthase medical term. What does prostaglandin endoperoxide synthase mean? ... Looking for online definition of prostaglandin endoperoxide synthase in the Medical Dictionary? ... prostaglandin endoperoxide synthase. Also found in: Dictionary, Thesaurus, Encyclopedia. prostaglandin endoperoxide synthase. [ ...
Prostaglandin H2 synthase 2 , Products for research use only! ... Prostaglandin G/H Synthase And Cyclooxygenase; Prostaglandin H2 ... ELISA Kit for Prostaglandin Endoperoxide Synthase 2 (PTGS2). Enzyme-linked immunosorbent assay for Antigen Detection.. ... Monoclonal Antibody to Prostaglandin Endoperoxide Synthase 2 (PTGS2). PGG/HS; PGHS2; PHS2; HCox2; COX2; Cyclooxygenase 2; ... Recombinant Prostaglandin Endoperoxide Synthase 2 (PTGS2). Positive Control; Immunogen; SDS-PAGE; WB.. ...
Human Prostaglandin Endoperoxide Synthase 2 (PTGS2) ELISA Kit. SEA699Hu-10x96wellstestplate Cloud-Clone 10x96-wells test plate ... Mouse Prostaglandin Endoperoxide Synthase 2 (PTGS2) ELISA Kit. SEA699Mu-10x96wellstestplate Cloud-Clone 10x96-wells test plate ... Should the Mouse Prostaglandin Endoperoxide Synthase 2 (PTGS2) ELISA Kit is proven to show malperformance, you will receive a ... Should the Mouse Prostaglandin Endoperoxide Synthase 2 (PTGS2) ELISA Kit is proven to show malperformance, you will receive a ...
A fluorescence microscopy method for quantifying the detection of prostaglandin endoperoxide H synthase-1 and CD-41 in MEG-01 ...
Yokoyama C, Takai T, Tanabe T. Primary structure of sheep prostaglandin endoperoxide synthase deduced from cDNA sequence. FEBS ... Yokoyama, C., Takai, T., & Tanabe, T. (1988). Primary structure of sheep prostaglandin endoperoxide synthase deduced from cDNA ... Primary structure of sheep prostaglandin endoperoxide synthase deduced from cDNA sequence. Chieko Yokoyama, Toshiyuki Takai, ... Yokoyama, C, Takai, T & Tanabe, T 1988, Primary structure of sheep prostaglandin endoperoxide synthase deduced from cDNA ...
... and questions answered by our Genetic and Rare Diseases Information Specialists for PROSTAGLANDIN-ENDOPEROXIDE SYNTHASE ... PROSTAGLANDIN-ENDOPEROXIDE SYNTHASE DEFICIENCY Title Other Names:. PTGS DEFICIENCY; PLATELET CYCLOOXYGENASE DEFICIENCY; ...
Nitric Oxide Synthase / metabolism* * Nitroarginine / pharmacology * Prostaglandin-Endoperoxide Synthases / metabolism* * ... Activation of protease-activated receptor 2 mediates cutaneous vasodilatation but not sweating: roles of nitric oxide synthase ... activation of PAR2 elicits cutaneous vasodilatation partly through nitric oxide synthase-dependent mechanisms, but does not ... that activation of PAR2 directly stimulates cutaneous vasodilatation and sweating via actions of nitric oxide synthase (NOS) ...
In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays ... Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive ... prostaglandin-endoperoxide synthase activity Source: UniProtKB-EC. Complete GO annotation on QuickGO ... ... Prostaglandin G/H synthase 1Add BLAST. 576. Amino acid modifications. Feature key. Position(s). DescriptionActions. Graphical ...
Autocatalytic tyrosine nitration of prostaglandin endoperoxide synthase-2 in LPS-stimulated RAW 264.7 macrophages ... detected a major nitrotyrosine positive protein band around 72 kDa and identified it as prostaglandin endoperoxide synthase-2 ( ... Under inflammatory conditions, nitrite formed via NO-synthase-2 may therefore act as an endogenous regulator for PGHS-2 in ...
In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays ... Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive ... prostaglandin-endoperoxide synthase activity Source: CAFA ,p>Inferred from Mutant Phenotype,/p> ,p>Describes annotations that ... "Tyrosine 385 of prostaglandin endoperoxide synthase is required for cyclooxygenase catalysis.". Shimokawa T., Kulmacz R.J., ...
Immunopresence and functional activity of prostaglandin-endoperoxide synthases and nitric oxide synthases in bovine corpora ... Immunopresence and functional activity of prostaglandin-endoperoxide synthases and nitric oxide synthases in bovine corpora ... The aim of this study was to evaluate the occurrence and the activity of prostaglandin-endoperoxide synthase 1 (PTGS1), PTGS2, ... The aim of this study was to evaluate the occurrence and the activity of prostaglandin-endoperoxide synthase 1 (PTGS1), PTGS2, ...
... which include prostaglandins, leukotrienes, thromboxanes, and lipoxins, are derived from the oxygenation of 20-carbon ... Biochemistry of prostaglandin endoperoxide H synthase-1 and synthase-2 and their differential susceptibility to nonsteroidal ... Prostaglandin endoperoxide H synthases-1 and -2. Adv Immunol. 1996. 62:167-215. [Medline]. ... Alterations in cellular adhesion and apoptosis in epithelial cells overexpressing prostaglandin endoperoxide synthase 2. Cell. ...
As ibuprofen acts specifically on COX sites of prostaglandin H2 synthase (prostaglandin endoperoxide synthase or prostaglandin ... BZW1, basic leucine zipper and W2 domains 1; GUSB, β-glucuronidase; PTGS, prostaglandin-endoperoxide synthase. *P ≤ 0.05, **P ... the global prostaglandin synthesis was evaluated immediately afterward with a Prostaglandin Screening ELISA Kit (Cayman ... the suppression of androgens and prostaglandins occurred in parallel, and, because for several decades prostaglandins have been ...
Prostaglandin Endoperoxide Synthases. p. 163. Introduction. p. 164. PGH Synthase Isozymes. p. 167. ...
Modulation of the prostaglandin-endoperoxide synthase 2 gene expression by variant haplotypes: influence of the 3′-untranslated ... Modulation of the prostaglandin-endoperoxide synthase 2 gene expression by variant haplotypes: influence of the 3′-untranslated ... Modulation of the prostaglandin-endoperoxide synthase 2 gene expression by variant haplotypes: influence of the 3′-untranslated ... Modulation of the prostaglandin-endoperoxide synthase 2 gene expression by variant haplotypes: influence of the 3′-untranslated ...
Prostaglandin endoperoxide H synthases-1 and -2. Adv Immunol 1996. 62:167-215. View this article via: PubMed CrossRef Google ... Prostaglandin synthase 2 gene disruption causes severe renal pathology in the mouse. Cell 1995. 83:473-482. View this article ... Expression of a mitogen-responsive gene encoding prostaglandin synthase is regulated by mRNA splicing. Proc Natl Acad Sci USA ... Primary structure of prostaglandin G/H synthase from sheep vesicular gland determined from the complementary DNA sequence. Proc ...
  • PTGS2 (COX-2), converts arachidonic acid (AA) to prostaglandin endoperoxide H2. (wikipedia.org)
  • Prostaglandin endoperoxide synthase 2 (PTGS2) and prostaglandins F2α and E2 synthases (PGFS and PGES) expression and prostaglandin F2α and E2 secretion following oestrogen and/or progesterone stimulation of the feline endometrium. (uzh.ch)
  • In this study, we investigated the mRNA expression of three genes involved in arachidonic acid (AA) metabolism and hence PG production in domestic cats: PG-endoperoxide synthase (PTGS2), PGF(2α) synthase (PGFS) and PGE(2) synthase (PGES). (uzh.ch)
  • The enzyme responsible for the conversion of arachidonic acid to prostaglandins in response to inflammation is prostaglandin endoperoxide synthase 2/cyclo-oxygenase 2 (PTGS2/COX2). (biomedcentral.com)
  • PTGS2 is a protein that is expressed as part of the acute response to inflammation [ 11 ] and is the main enzyme responsible for transforming arachidonic acid into prostaglandins. (biomedcentral.com)
  • Should the Mouse Prostaglandin Endoperoxide Synthase 2 (PTGS2) ELISA Kit is proven to show malperformance, you will receive a refund or a free replacement. (pharmas-eu.org)
  • Description: A sandwich quantitative ELISA assay kit for detection of Mouse Prostaglandin Endoperoxide Synthase 2 (PTGS2) in samples from serum, plasma or other biological fluids. (pharmas-eu.org)
  • Description: This is Double-antibody Sandwich Enzyme-linked immunosorbent assay for detection of Human Prostaglandin Endoperoxide Synthase 2 (PTGS2) in serum, plasma, tissue homogenates and other biological fluids. (pharmas-eu.org)
  • The aim of this study was to evaluate the occurrence and the activity of prostaglandin-endoperoxide synthase 1 (PTGS1), PTGS2, and endothelial, neuronal, and inducible nitric oxide synthase (e-, n-, and iNOS) in early, mid, late, and regressive corpora lutea (CL) of bovines during diestrus. (viamedica.pl)
  • Cycloxigenase-2 is encoded by the prostaglandin-endoperoxide synthase 2 (PTGS2) gene, which presents sequence variations in the promoter region (PR) and in the 3′-untranslated region (3′-UTR). (figshare.com)
  • Conversion of arachidonate to prostaglandin H2 is mediated by 2 different isozymes: the constitutive PTGS1 and the inducible PTGS2. (uniprot.org)
  • Prostaglandin-endoperoxide synthase 2 (PTGS2) gene polymorphisms and risk of biliary tract cancer and gallstones: a population-based study in Shang. (cdc.gov)
  • Although the mechanisms by which NSAIDs lower cancer risk remain unclear, NSAIDs reduce prostaglandin production by blocking prostaglandin-endoperoxide synthase 2 (PTGS2, commonly known as COX-2), an enzyme induced by proinflammatory stimuli that is often overexpressed in malignant tissue. (cdc.gov)
  • Prostaglandin endoperoxide synthases (also referred to as COX) are the rate-limiting enzymes in the conversion of arachidonic acid, a product of damaged cell membranes, into prostaglandins and they exist in at least 2 isoforms, PTGS1 (COX-1), and PTGS2 (COX-2). (aacrjournals.org)
  • PTGS2 is responsible for production of inflammatory prostaglandins. (drugbank.ca)
  • In cancer cells, PTGS2 is a key step in the production of prostaglandin E2 (PGE2), which plays important roles in modulating motility, proliferation and resistance to apoptosis. (drugbank.ca)
  • The enzymes cyclooxygenase -1 and -2 (i.e. prostaglandin G/H synthase 1 and 2 { PTGS1 and PTGS2 }) metabolize arachidonic acid to Prostaglandin G2 and prostaglandin H2 , which in turn may be converted to various prostaglandins , to prostacyclin , to thromboxanes , and to the 17-carbon product of thromboxane metabolism of prostaglandin G2/H2, 12-Hydroxyheptadecatrienoic acid (12-HHT). (wikipedia.org)
  • Prostaglandin-endoperoxide synthase (PTGS), also known as cyclooxygenase, is the key enzyme in prostaglandin biosynthesis, and acts both as a dioxygenase and as a peroxidase. (nih.gov)
  • Prostaglandin endoperoxide synthase 2, also referred to as cyclooxygenase 2 (COX-2), is a key enzyme in the conversion of arachidonic acid to prostaglandins and other eicosanoids. (nih.gov)
  • Prostaglandin-endoperoxide synthase (PTGS), also known as cyclooxygenase or COX , is a rate - limiting enzyme in the conversion of arachidonic acid, a product of damaged cell membranes, into prostaglandins. (wikigenes.org)
  • Cyclooxygenase 1 mediates prostaglandin synthesis and is modulated by anti inflammatory nonsteroidal drugs. (sigmaaldrich.com)
  • Cyclooxygenase 1 from sheep has been used as positive control protein in western blot analysis of osteoarthritis samples and in prostaglandin synthase activity assay. (sigmaaldrich.com)
  • Cyclooxygenase-2 induces angiogenesis in pancreatic cancer mediated by prostaglandin E 2 . (medscape.com)
  • The conversion of arachidonate to prostaglandin H2 is a 2 step reaction: a cyclooxygenase (COX) reaction which converts arachidonate to prostaglandin G2 (PGG2) and a peroxidase reaction in which PGG2 is reduced to prostaglandin H2 (PGH2). (uniprot.org)
  • They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins. (ebi.ac.uk)
  • To examine the role of cyclooxygenase (COX) isozymes in prostaglandin formation and oxidant stress in inflammation, we administered to volunteer subjects placebo or bolus injections of lipopolysaccharide (LPS), which caused a dose-dependent increase in temperature, heart rate, and plasma cortisol. (jci.org)
  • BACKGROUND: Prostaglandin endoperoxide synthase/cyclooxygenase (COX) is the key enzyme in gastric mucosal protection and repair but its cellular localisation in the human stomach is still unclear. (biomedsearch.com)
  • Cyclooxygenase (COX), officially known as prostaglandin-endoperoxide synthase (PTGS), is an enzyme (specifically, a family of isozymes, EC 1.14.99.1) that is responsible for formation of prostanoids, including thromboxane and prostaglandins such as prostacyclin, from arachidonic acid. (wikipedia.org)
  • 1 The biosynthesis of PGE 2 requires 3 sequential steps of the cyclooxygenase pathway: the release of arachidonic acid from membrane glycerophospholipids by phospholipase A 2 , conversion of arachidonic acid to the unstable intermediate PGH 2 by cyclooxygenase-1 or cyclooxygenase-2, and isomerization of PGH 2 to PGE 2 by PGE synthase (PGES). (ahajournals.org)
  • The critical step in the formation of proinflammatory PGs is the oxygenation of free AA by cyclooxygenase (COX) enzymes (also named PGH synthase or PG endoperoxide synthase), ( 27 ). (jimmunol.org)
  • Inducible vascular prostaglandin E 2 (PGE 2 ) synthesis by endothelial (ECs) and/or perivascular cells (PVCs) (a macrophage-derived vascular cell type) is implicated in the engagement of HPA and other CNS responses, by virtue of their capacity to express cyclooxygenase-2 (COX-2) and microsomal PGE 2 synthase-1. (jneurosci.org)
  • Ascorbic acid enhances the inhibitory effect of aspirin on neuronal cyclooxygenase-2-mediated prostaglandin E2 production. (cogprints.org)
  • Inhibition of neuronal cyclooxygenase-2 (COX-2) and hence prostaglandin E2 (PGE2) synthesis by non-steroidal anti-inflammatory drugs has been suggested to protect neuronal cells in a variety of pathophysiological situations including Alzheimer's disease and ischemic stroke. (cogprints.org)
  • A series of prostaglandins F 2 -like compounds are produced in vivo in human by a non-cyclooxygenase, free radical-catalyzed mechanism. (springer.com)
  • Pratico D, Lawson JA, FitzGerald GA. Cyclooxygenase-dependent formation of the isoprostane, 8-epi Prostaglandin F 2α . (springer.com)
  • The vascular endothelium manufactures prostaglandin E 2 (PGE 2 ) and/or I 2 (PGI 2 ) via a pathway that involves oxygenation of arachidonic acid by cyclooxygenase (COX)-1 and -2. (ahajournals.org)
  • Differential inhibition of prostaglandin endoperoxide synthase (cyclooxygenase) isozymes by aspirin and other non-steroidal anti-inflammatory drugs. (thefreedictionary.com)
  • In addition, the endotoxin-induced expression of the inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2 proteins was investigated in a mouse macrophage cell line (RAW 264.7) treated with ACE in vitro, to clarify the anti-inflammatory effect. (arvojournals.org)
  • They are cyclooxygenase 1 (COX-1), cyclooxygenase 2 ( COX-2 ) and prostaglandin E synthase (PGES). (ndif.org)
  • Prostaglandin (PGs) is regulated by arachidonic acid (AA) release by phospholipase A2 (PLA2) and its conversion to PGs by cyclooxygenase (COX). (semanticscholar.org)
  • Activation of cytosolic phospholipase A2 by platelet-derived growth factor is essential for cyclooxygenase-2-dependent prostaglandin E2 synthesis in mouse osteoblasts cultured with interleukin-1. (semanticscholar.org)
  • IL-13 and IL-4 inhibit bone resorption by suppressing cyclooxygenase-2-dependent prostaglandin synthesis in osteoblasts. (semanticscholar.org)
  • It is involved in the conversion of arachidonic acid to prostaglandin H2 , an important precursor of prostacyclin , among others. (wikipedia.org)
  • The PTGS (COX) enzymes catalyze the conversion of arachidonic acid to prostaglandins in two steps. (wikipedia.org)
  • COX-1 catalyzes the conversion of arachidonic acid to prostaglandin H 2 (the first step in the biosynthesis of prostaglandins, thromboxanes, and prostacyclins). (sigmaaldrich.com)
  • COX-2 catalyzes the transformation of arachidonic acid to prostaglandin H2, which is the rate-limiting step in the formation of prostaglandins (PGs) and thromboxane A2 (TXA2). (atlasgeneticsoncology.org)
  • Cyclooxygenases are key enzymes required for prostaglandin (PG) synthesis, converting the arachidonic acid (AA) released by phospholipase A2 into prostaglandins. (nih.gov)
  • A compound or agent that combines with cyclooxygenases (EC 1.14.99.1) and thereby prevents its substrate-enzyme combination with arachidonic acid and the formation of icosanoids, prostaglandins, and thromboxanes. (ebi.ac.uk)
  • The specific reaction catalyzed is the conversion from arachidonic acid to Prostaglandin H2, via a short-living Prostaglandin G2 intermediate. (wikipedia.org)
  • In LES circular muscle a low molecular weight pancreatic-like phospholipase A 2 ( group I PLA 2 ) causes production of arachidonic acid, which is metabolized to prostaglandins and thromboxanes. (nature.com)
  • Prostaglandin (PG) E 2 is a major product of arachidonic acid metabolism, being implicated in pain and inflammatory responses, as well as in the regulation of various physiological functions. (ahajournals.org)
  • The Cox-2 enzyme is important for the conversion of arachidonic acid to prostaglandins and is associated with edema, inflammatory infiltrate, fever, and pain. (asm.org)
  • The anti-inflammatory effects of ketoprofen are believed to be due to inhibition cylooxygenase-2 (COX-2), an enzyme involved in prostaglandin synthesis via the arachidonic acid pathway. (drugbank.ca)
  • PG endoperoxidase H synthases (PGHSs), also called cyclooxygenases (Cox), are the rate-limiting enzymes that initiate conversion of arachidonic acid to all PGs, prostacyclins, and thromboxanes ( 2 ). (rupress.org)
  • Arachidonic acid (AA), formed from membrane phospholipids by the action of phospholipase A 2 , is the principal substrate for cyclooxygenases (COXs), which catalyze the rate-limiting conversion of AA to prostaglandin H 2 (PGH 2 ). (jneurosci.org)
  • Arachidonic acid is converted enzymatically into different prostaglandins (PG) by the activity of a key enzyme, PG-endoperoxide synthase (PGHS), which exhibits both bisoxygenase and peroxidase activity (1). (springer.com)
  • 1-3 Angiotensin (Ang) II acutely stimulates prostaglandin synthesis in endothelial cells by promoting phospholipase-catalyzed deacylation of arachidonic acid, and thus increasing the amount of arachidonic acid available to COX, and also may induce COX-2 expression. (ahajournals.org)
  • The conversion of arachidonic acid (20:4) to cyclic endoperoxide ([PGG. (thefreedictionary.com)
  • The cyclo-oxygenase (COX) enzymes are involved in numerous physiological responses including inflammation, where they catalyse the synthesis of prostaglandins (PGs) from arachidonic acid. (bmj.com)
  • Enzyme complexes that catalyze the formation of PROSTAGLANDINS from the appropriate unsaturated FATTY ACIDS, molecular OXYGEN, and a reduced acceptor. (curehunter.com)
  • COX2 is an enzyme that belongs to the prostaglandin G/H synthase family. (atlasgeneticsoncology.org)
  • The results were confirmed by digestion of the enzyme with carboxypeptidase Y and by automated Edman degradation of the intact enzyme polypeptide and peptide fragments obtained by limited proteolysis of the enzyme with Achromobacter proteinase I. Mature sheep prostaglandin endoperoxide synthase is shown to be composed of 576 amino acids with an M r of 66 175. (elsevier.com)
  • Prostaglandin endoperoxide synthase: regulation of enzyme expression. (springer.com)
  • 2.Electron microscopic immunocytochemistry demonstrated the colocalization of ATP synthase and cytochrome P-450 of side chain cleavage enzyme in the mitochondria of rat and bovine adrenocortical cells. (nii.ac.jp)
  • alias COX-2), and prostaglandin-E receptor-2 gene (PTGER2) and risk of atherothrombotic disorders. (ovid.com)
  • Although these prospective data implicate the potential involvement of prostaglandin-E receptor-2 gene variation in atherothrombosis, external validation of our findings is needed. (ovid.com)
  • prostaglandin-endoperoxide-synthase-2 [gene contains] a canonical TATA box (nucleotide residues at positions -31 to -25 for the human gene). (wikiversity.org)
  • Upregulation of HO-1 gene expression by retrovirus-mediated delivery of the human HO-1 gene also attenuated heme and Ang II-induced prostaglandin synthesis. (ahajournals.org)
  • We tested this hypothesis by examining the effect of interventions that suppress HO activity, or induce HO-1 gene expression, on Ang II-induced prostaglandin synthesis in cultures of human femoral endothelial cells. (ahajournals.org)
  • It has been shown that IRF-1-deficient cells exhibit impaired induction of several genes involved in the innate immune response, including the 2-5A synthetase ( 11 ), inducible nitric oxide synthase (iNOS [12]), and IL-12 p40 and p35 genes ( 13 ). (rupress.org)
  • Publications] Tamura,M.: 'Coexistence of nitric oxide synthase,tyrosine hydroxylase and Vascactive intestinal polypeptide in human penile tissue. (nii.ac.jp)
  • The resulting inhibition of prostaglandin and thromboxane synthesis has the effect of reduced inflammation, as well as antipyretic, antithrombotic and analgesic effects. (wikipedia.org)
  • Material: Data for oral potencies of 24 NSAIDs in rats were collected from the literature and from New Drug Applications with respect to the following parameters: antiinflammatory, analgesic, antipyretic, acute ulcerogenic activities, acute toxicity, in vitro inhibition of prostaglandin synthesis, acid dissociation constant (pK a ), octanolwater partition coefficient and elimination half-life. (springer.com)
  • Vane JR. Inhibition of prostaglandin synthesis as a mechanism of action of aspirin like drugs. (springer.com)
  • Aspirin-like drugs may block pain independently of prostaglandin synthesis inhibition. (springer.com)
  • The inhibition of IL-1beta-mediated PGE2 synthesis by ascorbic acid was not due to the inhibition of the expression of COX-2 or microsomal prostaglandin E synthase (mPGES-1). (cogprints.org)
  • Aspirin inhibition and acetylation of the plant cytochrome P450, allene oxide synthase, resembles that of animal prostaglandin endoperoxide H synthase. (thefreedictionary.com)
  • In vitro inhibition and stimulation of purified prostaglandin endoperoxide synthase by flavonoids: Structure-activity relationship. (thefreedictionary.com)
  • In endotoxin-stimulated RAW 264.7 macrophages, we have detected a major nitrotyrosine positive protein band around 72 kDa and identified it as prostaglandin endoperoxide synthase-2 (PGHS-2). (hacettepe.edu.tr)
  • The results presented here identify for the first time a T. brucei protein that exhibits a PGF synthase activity capable of specifically converting PGH 2 to PGF 2α . (rupress.org)
  • In this study, we demonstrate that interferon (IFN)-γ alone or in synergy with lipopolysaccharide (LPS) or interleukin 1α induces Cox-2 expression in mouse peritoneal macrophages, which is paralleled by changes in Cox-2 protein levels and prostaglandin E 2 (PGE 2 ) release. (rupress.org)
  • Picot D, Loll PJ, Garavito MR. The X-ray crystal srtucture of the menbrane protein prostaglandin H 2 synthase-1. (springer.com)
  • ST NetWatch: Protein Databases Arquivado 02 de xuño de 2013 en Wayback Machine . (wikipedia.org)
  • After 24 hours, the aqueous humor was collected from both eyes, and the number of infiltrating cells, protein concentration, nitric oxide (NO), prostaglandin (PG)-E2, and TNF-α levels in the aqueous humor were determined. (arvojournals.org)
  • Activation of HIMECs by VEGF resulted in enhanced expression of cyclo-oxygenase-2 (COX-2) mRNA, protein and prostaglandin E 2 (PGE 2 ) production. (bmj.com)
  • The synthesized PGH2 is converted to prostaglandins ( PGD2 , PGE2 , PGF 2α ), prostacyclin (PGI2), or thromboxane A2 by tissue-specific isomerases. (wikipedia.org)
  • In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays an important role in cytoprotection. (uniprot.org)
  • Rather, ascorbic acid dose-dependently (0.1-100 microM) produced a significant reduction in IL-1beta-mediated production of 8-iso-prostaglandin F2alpha (8-iso-PGF2alpha), a reliable indicator of free radical formation, suggesting that the effects of ascorbic acid on COX-2-mediated PGE2 biosynthesis may be the result of the maintenance of the neuronal redox status since COX activity is known to be enhanced by oxidative stress. (cogprints.org)
  • PGE2 is the main kidney prostaglandin and is thought to be mainly produced in the kidney inner medulla (IM). (ndif.org)
  • We hypothesize that the expression of the major PGE2 synthesis enzymes cyclooxygenases 1 and 2 (COX-1, COX-2 ) and membrane -associated PGE2 synthase (mPGES) is altered in the kidneys of rats with NDI and CDI . (ndif.org)
  • We have reported that cadmium (Cd) stimulates bone resorption via prostaglandin E2 (PGE2), which is mainly produced in osteoblasts. (semanticscholar.org)
  • prostaglandin biosynthesis. (abcam.com)
  • Prostaglandin and thromboxane biosynthesis. (springer.com)
  • Among them, prostaglandin endoperoxide synthases (cyclooxygenases) catalyze the committed step that leads to prostaglandin biosynthesis [ 12 - 14 ]. (hindawi.com)
  • 3 The Occurence of Thromboxane Synthase in Tumor Cells. (weltbild.de)
  • The eicosanoids, which include prostaglandins, leukotrienes, thromboxanes, and lipoxins, are derived from the oxygenation of 20-carbon polyunsaturated essential fatty acids via the COX and lipoxygenase pathways. (medscape.com)
  • Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. (uniprot.org)
  • Cell-specific isomerization or reduction of PGH2 by various synthases (isomerases) or reductases leads to the formation of different prostanoids (2). (springer.com)
  • These results indicate that overexpression of the HO system exerts an inhibitory influence on Ang II-induced synthesis of prostaglandins by endothelial cells. (ahajournals.org)
  • The most frequent adverse effect of NSAIDs is irritation of the gastric mucosa as prostaglandins normally have a protective role in the gastrointestinal tract. (wikipedia.org)
  • Ketoprofen has pharmacologic actions similar to those of other prototypical NSAIDs, which inhibit prostaglandin synthesis. (drugbank.ca)
  • The relative anti-inflammatory activities of the immunomodulators HR325 and leflunomide, or its active metabolite A77 1726, were examined by determining potencies in vitro on prostaglandin endoperoxide H synthase (PGHS) and in vivo in rat air pouch inflammation. (aspetjournals.org)
  • Prostaglandins are integral components in the cellular response to inflammation, promoting cellular proliferation and angiogenesis. (biomedcentral.com)
  • This results in decreased levels of prostaglandins that mediate pain, fever and inflammation. (drugbank.ca)
  • The names "prostaglandin synthase (PHS)", "prostaglandin synthetase (PHS)", and "prostaglandin-endoperoxide synthetase (PES)" are older terms still sometimes used to refer to COX. (wikipedia.org)
  • Under inflammatory conditions, nitrite formed via NO-synthase-2 may therefore act as an endogenous regulator for PGHS-2 in stimulated macrophages. (hacettepe.edu.tr)
  • Normal mouse epidermis constitutively expresses prostaglandin-H synthase 1 (PGHS-1) but no PGHS-2. (portlandpress.com)
  • abstract = "The complete amino acid sequence of prostaglandin endoperoxide synthase from sheep vesicular gland has been deduced by cloning and sequence analysis of DNA complementary to its messenger RNA. (elsevier.com)
  • Sex steroids in synergy with prostaglandins (PG) are involved in the regulation of cyclic ovarian function. (uzh.ch)
  • We are defining the regulation and role of the prostaglandin (PG)F2a receptor (FP) in the control of parturition at term and preterm. (ualberta.ca)
  • The present study examined the role and mechanism of microsomal PG synthase-1 (mPGES-1) in vascular response to angiotensin II (Ang II) infusion. (ahajournals.org)
  • Microsomal PGE 2 synthase-1 (mPGES-1) is the dominant and best-studied terminal PGE 2 synthase in brain. (jneurosci.org)
  • Mediates the formation of prostaglandins from arachidonate. (abcam.com)
  • Subsequently, the resulting PGH 2 is converted in vivo and in vitro to various arachidonate metabolites, such as PGD 2 , PGE 2 , and PGF 2α ( Fig. 1 ) by the action of their respective synthases ( 1 ). (rupress.org)
  • ANGPTL4 induction by prostaglandin E2 under hypoxic conditions promotes colorectal cancer progression. (mayo.edu)
  • Transcriptional induction of prostaglandin G/H synthase-2 by basic fibroblast growth factor. (semanticscholar.org)
  • We hypothesize that the status of the endothelial HO system influences the angiotensin (Ang) II-induced increase in the endothelial production of prostaglandin I 2 (PGI 2 ) (measured as 6-keto-PGF 1α ) and prostaglandin E 2 (PGE 2 ), eicosanoids that modulate the vascular actions of Ang II. (ahajournals.org)
  • Effects of progesterone and estradiol on prostaglandin endoperoxide synthase in ovine endometrial tissue. (thefreedictionary.com)
  • Cadmium stimulates prostaglandin E2 synthesis in osteoblast-like cells, MC3T3-E1. (semanticscholar.org)
  • Abayasekara DRE, Wathes DC (1999) Effects of altering dietary fatty acid composition on prostaglandin synthesis and fertility. (springer.com)
  • Publications] Yoshinaga-Hirabayashi,H: 'Electron microscopic immunocytochemistry on the colocalization of ATP-synthase and cytochrome P-450 of side-chain cleavage enzymes' Arch.Histol.Cytol.56. (nii.ac.jp)
  • This effect of Ang II on prostaglandin production by endothelial cells was attenuated in cells treated with SnCl 2 (10 μmol/L), an inducer of HO-1, but was magnified in cells treated with the HO inhibitor ZnDPP or heme. (ahajournals.org)
  • Of note, prostaglandin synthesis by lysates of endothelial cells stimulated with heme or Ang II appear to involve COX-2, because it was blunted by NS-398, which is presumed to inhibit COX-2 specifically. (ahajournals.org)
  • 6 According to a recent study, prostaglandin synthesis in rabbit coronary and human endothelial cells decreases in response to interventions that upregulate the expression of heme oxygenase (HO)-1. (ahajournals.org)
  • 3.Prostaglandin endoperoxide synthase was immunolocalized in mast cells, smooth muscle cells of muscularis mucosae and inner muscle layr, endothelial cells of arteries, nerve cells of myenteric plexus and perioneal epithelial cells of bovine intestines. (nii.ac.jp)
  • Determinants of the cellular specificity of acetaminophen as an inhibitor of prostaglandin H(2) synthases. (cogprints.org)
  • The membrane binding domains of prostaglandin endoperoxide H synthases 1 and 2. (wikipedia.org)
  • These acids can be turned into some anti-inflammatory prostacyclins by COX instead of pro-inflammatory prostaglandins. (wikipedia.org)
  • Tissue-specific prostaglandin synthases convert PGH 2 into different prostanoids. (jneurosci.org)
  • Lipolysaccaride-induced expression of prostaglandin H synthase-2 in alveolar macrophages is inhibited by dexamethasone but not by aspirin. (springer.com)
  • 12,13 It is conceivable, then, that Ang II-mediated upregulation of HO-1 creates a setting that does not favor Ang II-induced stimulation of prostaglandin synthesis. (ahajournals.org)
  • Publications] Ishimura,K.: 'Immunocytochemical localization of prostaglandin endoperoxide synthase in the bovine intestine. (nii.ac.jp)
  • Publications] K.Ishimura, T.Suzuki, K.Fukui, A.Yamamoto, Y.Omoto, N.Ueda and S.Yamamoto: 'Immunocytochemical localization of prostaglandin endoperoxide synthase in the bovine intestine. (nii.ac.jp)
  • The Ang II infusion induced mRNA expression of mPGES-1, as well as mPGES-2 and cytosolic PGE synthase in the aortas as assessed by real-time RT-PCR. (ahajournals.org)
  • the hydroperoxidase activity uses glutathione to convert prostaglandin G 2 to prostaglandin H 2 . (thefreedictionary.com)