General Information of the Protein
Protein ID |
PT00940
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Protein Name |
Prostaglandin G/H synthase 1
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Secondarily Protein Name |
Cyclooxygenase-1
Prostaglandin H2 synthase 1
Prostaglandin-endoperoxide synthase 1
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Gene Name |
PTGS1
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Secondarily Gene Name |
COX1
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Sequence |
MSRSLLLWFLLFLLLLPPLPVLLADPGAPTPVNPCCYYPCQHQGICVRFGLDRYQCDCTRTGYSGPNCTIPGLWTWLRNSLRPSPSFTHFLLTHGRWFWEFVNATFIREMLMRLVLTVRSNLIPSPPTYNSAHDYISWESFSNVSYYTRILPSVPKDCPTPMGTKGKKQLPDAQLLARRFLLRRKFIPDPQGTNLMFAFFAQHFTHQFFKTSGKMGPGFTKALGHGVDLGHIYGDNLERQYQLRLFKDGKLKYQVLDGEMYPPSVEEAPVLMHYPRGIPPQSQMAVGQEVFGLLPGLMLYATLWLREHNRVCDLLKAEHPTWGDEQLFQTTRLILIGETIKIVIEEYVQQLSGYFLQLKFDPELLFGVQFQYRNRIAMEFNHLYHWHPLMPDSFKVGSQEYSYEQFLFNTSMLVDYGVEALVDAFSRQIAGRIGGGRNMDHHILHVAVDVIRESREMRLQPFNEYRKRFGMKPYTSFQELVGEKEMAAELEELYGDIDALEFYPGLLLEKCHPNSIFGESMIEIGAPFSLKGLLGNPICSPEYWKPSTFGGEVGFNIVKTATLKKLVCLNTKTCPYVSFRVPDASQDDGPAVERPSTEL
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Organism |
Homo sapiens, Human
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Protein Classification |
Enzyme
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Oxidoreductase
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Function |
Dual cyclooxygenase and peroxidase that plays an important role in the biosynthesis pathway of prostanoids, a class of C20 oxylipins mainly derived from arachidonate ((5Z,8Z,11Z,14Z)-eicosatetraenoate, AA, C20:4(n-6)), with a particular role in the inflammatory response. The cyclooxygenase activity oxygenates AA to the hydroperoxy endoperoxide prostaglandin G2 (PGG2), and the peroxidase activity reduces PGG2 to the hydroxy endoperoxide prostaglandin H2 (PGH2), the precursor of all 2-series prostaglandins and thromboxanes. This complex transformation is initiated by abstraction of hydrogen at carbon 13 (with S-stereochemistry), followed by insertion of molecular O2 to form the endoperoxide bridge between carbon 9 and 11 that defines prostaglandins. The insertion of a second molecule of O2 (bis-oxygenase activity) yields a hydroperoxy group in PGG2 that is then reduced to PGH2 by two electrons (PubMed:7947975). Involved in the constitutive production of prostanoids in particular in the stomach and platelets. 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. In platelets, it is involved in the generation of thromboxane A2 (TXA2), which promotes platelet activation and aggregation, vasoconstriction and proliferation of vascular smooth muscle cells (Probable). Can also use linoleate (LA, (9Z,12Z)-octadecadienoate, C18:2(n-6)) as substrate and produce hydroxyoctadecadienoates (HODEs) in a regio- and stereospecific manner, being (9R)-HODE ((9R)-hydroxy-(10E,12Z)-octadecadienoate) and (13S)-HODE ((13S)-hydroxy-(9Z,11E)-octadecadienoate) its major products (By similarity).
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Uniprot ID |
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Subcellular Location |
Microsome membrane
Endoplasmic reticulum membrane
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Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein Protein Cell Line Compound Bioactivity Value: <= 0.1 μM > 0.1 μM and <= 10 μM > 10 μM Imprecise Activity |
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Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000011 , CHO
Cell Line ID: CL000880 , COS
Cell Line ID: CL000249 , OVCAR-3
Cell Line ID: CL000013 , Sf9
Cell Line ID: CL000058 , T-REx-293
Cell Line ID: CL000100 , U-937
Biochemical Assays
Clinical Information about the Protein
Target 1 ( Prostaglandin G/H synthase 1 (COX-1) )
Target Type | Successful Target | ||||
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Disease | 19 Target-related Diseases | 19 | |||
1 | Pulmonary and extrapulmonary tuberculosis [ICD-11: 1B10.Z] | ||||
2 | Inflammatory bowel disease [ICD-11: DD72] | ||||
3 | Postoperative inflammation [ICD-11: 1A00-CA43.1] | ||||
4 | Hypertriglyceridemia [ICD-11: 5C80.1] | ||||
5 | Arthritis [ICD-11: FA20] | ||||
6 | Dysmenorrhea [ICD-11: GA34.3] | ||||
7 | Malnutrition [ICD-11: 5B50-5B71] | ||||
8 | Ulcerative colitis [ICD-11: DD71] | ||||
9 | Osteoarthritis [ICD-11: FA00-FA05] | ||||
10 | Pain [ICD-11: MG30-MG3Z] | ||||
11 | Seborrhoeic dermatitis [ICD-11: EA81] | ||||
12 | Rheumatoid arthritis [ICD-11: FA20] | ||||
13 | Miosis [ICD-11: LA11.62] | ||||
14 | Myalgia [ICD-11: FB56.2] | ||||
15 | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | ||||
16 | Duchenne dystrophy [ICD-11: 8C70] | ||||
17 | Gout [ICD-11: FA25] | ||||
18 | Analgesia [ICD-11: MB40.8] | ||||
19 | Giant cell arteritis [ICD-11: 4A44.2] | ||||
Approved Drug(s) | 14 Approved Drugs | 14 | |||
1 | Aminosalicylic Acid | Approved | |||
2 | Balsalazide | Approved | |||
3 | Bromfenac | Approved | |||
4 | Eicosapentaenoic acid/docosa-hexaenoic acid | Approved | |||
5 | FENBUFEN | Approved | |||
6 | Flufenamic Acid | Approved | |||
7 | Gamma-Homolinolenic acid | Approved | |||
8 | Meclofenamate Sodium | Approved | |||
9 | Mesalazine | Approved | |||
10 | Naproxen | Approved | |||
11 | Piroxicam | Approved | |||
12 | Salicyclic acid | Approved | |||
13 | Salsalate | Approved | |||
14 | Suprofen | Approved | |||
Clinical Trial Drug(s) | 4 Clinical Trial Drugs | 4 | |||
1 | (S)-FLURBIPROFEN | Preregistration | |||
2 | Curcumin | Phase 3 | |||
3 | EPICATECHIN | Phase 1/2 | |||
4 | Resveratrol | Phase 3 | |||
Discontinued Drug(s) | 4 Discontinued Drugs | 4 | |||
1 | INDOPROFEN | Withdrawn from market | |||
2 | Metamizole | Withdrawn from market | |||
3 | Phenacetin | Withdrawn from market | |||
4 | TEBUFELONE | Discontinued in Phase 2 |