Therapeutic Targets Database
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TTD Target ID: TTDS00040

Target Information
NameProstaglandin G/H synthase 1    
Type of targetSuccessful target    
SynonymsCOX-1    
Cyclooxygenase -1    
Cyclooxygenase-1    
PGH synthase 1    
PGHS-1    
PHS 1    
Prostaglandin H2 synthase 1    
Prostaglandin-endoperoxide synthase 1    
DiseaseCardiovascular disease, unspecified
[ICD9: 390-459   ICD10: I00-I99]
[1]
Chronic inflammatory diseases[2]
Drug(s)BalsalazideApprovedInflammatory bowel disease[3]
BromfenacApprovedPostoperative inflammation[4]
Gamma-Homolinolenic acidApprovedDietary shortage[5][6][7]
MesalazineApprovedUlcerative colitis[8]
Salicyclic acidApprovedAcne vulgaris[9]
SalsalateApprovedRheumatoid arthritis and osteoarthritis[10][11]
SuprofenApprovedMiosis during ocular surgery[12]
BioChemical ClassOxidoreductases acting on paired donors    
EC NumberEC 1.14.99.1
PathwayArachidonic acid metabolism
Metabolic pathways
UniProt IDP23219
FunctionMay play an important role in regulating or promoting cell proliferation in some normal and neoplastically transformed cells.    
SequenceMSRSLLLRFLLFLLLLPPLPVLLADPGAPTPVNPCCYYPCQHQGICVRFGLDRYQCDCTR TGYSGPNCTIPGLWTWLRNSLRPSPSFTHFLLTHGRWFWEFVNATFIREMLMRLVLTVRS NLIPSPPTYNSAHDYISWESFSNVSYYTRILPSVPKDCPTPMGTKGKKQLPDAQLLARRF LLRRKFIPDPQGTNLMFAFFAQHFTHQFFKTSGKMGPGFTKALGHGVDLGHIYGDNLERQ YQLRLFKDGKLKYQVLDGEMYPPSVEEAPVLMHYPRGIPPQSQMAVGQEVFGLLPGLMLY ATLWLREHNRVCDLLKAEHPTWGDEQLFQTTRLILIGETIKIVIEEYVQQLSGYFLQLKF DPELLFGVQFQYRNRIAMEFNHLYHWHPLMPDSFKVGSQEYSYEQFLFNTSMLVDYGVEA LVDAFSRQIAGRIGGGRNMDHHILHVAVDVIRESREMRLQPFNEYRKRFGMKPYTSFQEL VGEKEMAAELEELYGDIDALEFYPGLLLEKCHPNSIFGESMIEIGAPFSLKGLLGNPICS PEYWKPSTFGGEVGFNIVKTATLKKLVCLNTKTCPYVSFRVPDASQDDGPAVERPSTEL
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor (-)-3-O-acetylspectaline[13]
(11H-Dibenzo[b,e][1,4]dioxepin-2-yl)-acetic acid[14]
(11H-Dibenzo[b,e][1,4]dioxepin-7-yl)-acetic acid[14]
(11H-Dibenzo[b,e][1,4]dioxepin-8-yl)-acetic acid[14]
(3-Chloro-4-Propoxy-Phenyl)-Acetic Acid[15]
(R)-2-[16]
(S)-FLURBIPROFEN[16]
(Z)-2'-des-methyl sulindac sulfide[17]
1,2-dihydro-3- (2,3,4-trimethoxyphenyl)naphthalene[18]
1- (4-[19]
1- (4-[19]
1- (4-aminosulfonylphenyl)-2-[20]
1- (4-aminosulfonylphenyl)-2-[20]
2'-epi-guianin[21]
2,4'-Dimethoxy-5,3'-di- (2-propenyl)-biphenyl[22]
2- (1,1'-Biphenyl-4-Yl)Propanoic Acid[15]
2- (2,3,4-trimethoxyphenyl)-1H-indene[18]
2- (2-[23]
2- (2-Methylpropanoyl)-1,3,5-benzenetriol[24]
2- (2-methoxyphenyl)-1H-indene[18]
2- (3'-Allyl-biphenyl-4-yl)-propionic acid[25]
2- (3'-Ethyl-biphenyl-4-yl)-propionic acid[25]
2- (3'-Ethylsulfanyl-biphenyl-4-yl)-propionic acid[25]
2- (3'-Vinyl-biphenyl-4-yl)-propionic acid[25]
2- (3-Phenyl-propyl)-1,2-dihydro-indazol-3-one[26]
2- (N-[27]
2- (N-[27]
2- (p-Methylsulfonylbenzoyl)furan[28]
2-Benzyl-1,2-dihydro-indazol-3-one[26]
2-Bromoacetyl Group[29]
2-Furan-2-ylmethyl-1,2-dihydro-indazol-3-one[26]
2-Methyl-1,2-dihydro-indazol-3-one[26]
2-Naphthalen-2-ylmethyl-1,2-dihydro-indazol-3-one[26]
2-Phenethyl-1,2-dihydro-indazol-3-one[26]
2-Phenyl-1,2-dihydro-indazol-3-one[26]
2-[4- (1H-Indol-5-yl)-phenyl]-propionic acid[25]
3 beta-O-acetyloleanolic acid[30]
3- (4-Methanesulfonyl-phenyl)-1-phenyl-propynone[31]
4'-Methoxy-5,3'-dipropyl-biphenyl-2ol[22]
4,5-Bis (4-chlorophenyl)-1,2-selenazole[32]
4,5-Bis (4-chlorophenyl)isothiazole[33]
4,5-Bis (4-methoxyphenyl)-1,2-selenazole[32]
4,5-Bis (4-methoxyphenyl)-3H-1,2-dithiol-3-one[33]
4,5-Bis (4-methoxyphenyl)-3H-1,2-dithiole-3-thione[33]
4,5-Bis (4-methoxyphenyl)isothiazole[33]
4- (4-Chlorophenyl)-5-[33]
4- (4-Chlorophenyl)-5-p-tolyl-1,2-selenazole[32]
4- (4-Chlorophenyl)-5-p-tolyl-3H-1,2-dithiol-3-one[33]
4- (4-Chlorophenyl)-5-p-tolylisothiazole[33]
4- (5-[33]
4-amino-N- (2-chlorophenyl)benzenesulfonamide[34]
4-amino-N- (4-chlorophenyl)benzenesulfonamide[34]
4-amino-N-p-tolylbenzenesulfonamide[34]
5,3'-Dipropyl-biphenyl-2,4'-diol[22]
5- (2-1H-indenyl)-1,3-benzodioxole[18]
5- (2-Imidazol-1-yl-ethyl)-7,8-dihydro-quinoline[35]
5- (4-Chlorophenyl)-4-[33]
5- (4-Chlorophenyl)-4-p-tolyl-1,2-selenazole[32]
5- (4-Chlorophenyl)-4-p-tolyl-3H-1,2-dithiol-3-one[33]
5- (4-Chlorophenyl)-4-p-tolylisothiazole[33]
5- (4-Methoxyphenyl)-4-p-tolyl-1,2-selenazole[32]
5- (4-Methoxyphenyl)-4-p-tolylisothiazole[33]
5-Ethyl-3,4-diphenyl-isoxazole[36]
5-Methyl-3,4-diphenyl-isoxazole[36]
5-Phenyl-pentanoic acid benzyl-hydroxy-amide[37]
Acetic Acid Salicyloyl-Amino-Ester[15]
Acetic acid 2-hept-2-ynylsulfanyl-phenyl ester[38]
Acetic acid 2-hept-3-ynylsulfanyl-phenyl ester[38]
Acetic acid 2-heptylselanyl-phenyl ester[38]
Acetic acid 2-heptylsulfanyl-phenyl ester[38]
Acetic acid 2-hex-2-ynylsulfanyl-phenyl ester[38]
Acetic acid 2-hexylsulfanyl-phenyl ester[38]
Acetic acid 2-pentylsulfanyl-phenyl ester[38]
Alpha-D-Mannose[29]
Arachidonic Acid[29]
B-Octylglucoside[29]
BW-755C[39]
Balsalazide[3]
Beta-D-Glucose[29]
Beta-D-Mannose[29]
Bromfenac[4]
CATECHIN[40]
CATECHIN[40]
CIMICOXIB[41]
CURCUMIN[42]
DEMETHOXYCURCUMIN[42]
DOCOSAHEXAENOIC ACID[43]
EPICATECHIN[40]
EPICATECHIN[40]
FENBUFEN[44]
Flufenamic Acid[45]
Flurbiprofen Methyl Ester[29]
Gamma-Homolinolenic acid[5][6][7]
HONOKIOL[22]
Heme[15]
Hyperforin[46]
IMRECOXIB[47]
INDOPROFEN[16]
IODOINDOMETHACIN[48]
IODOSUPROFEN[48]
L-745337[49]
METHYLHONOKIOL[22]
Mesalazine[8]
N- (1H-indazol-5-yl)acetamide[50]
N- (3-[51]
N- (3-phenoxy-4-pyridinyl)ethanesulfonamide[52]
N- (3-phenoxy-4-pyridinyl)propanesulfonamide[52]
N- (3-phenoxypyridin-4-yl)methanesulfonamide[51]
N- (3-phenylamino-4-pyridinyl)methanesulfonamide[51]
O-Acetylserine[29]
Oxametacin[53]
P- (2'-Iodo-5'-Thenoyl)Hydrotropic Acid[15]
PHENIDONE[26]
Phenacetin[54]
Prifelone[55]
Primary alcohol metabolite of celecoxib[56]
Protoporphyrin Ix Containing Co[29]
R-KETOPROFEN[16]
RESORCINOL[40]
Resveratrol[1]
Resveratrol[57]
Resveratrol Potassium3-Sulfate[58]
Resveratrol Potassium4,-Sulfate[58]
SC-560[59]
SC-58451[60]
Salicyclic acid[9]
Salsalate[10][11]
Suprofen[12]
TEBUFELONE[61]
TENIDAP[62]
alpha-Methyl-4-biphenyl-acetic acid[48]
eicosapentaenoic acid[43]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
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Ref 2COX-1, COX-2, and COX-3 and the future treatment of chronic inflammatory disease. Lancet. 2000 Feb 19;355(9204):646-8. To Reference
Ref 3Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. To Reference
Ref 4Curr Med Res Opin. 2006 Jun;22(6):1133-40.Comparison of cyclooxygenase inhibitory activity and ocular anti-inflammatory effects of ketorolac tromethamine and bromfenac sodium. To Reference
Ref 5Differential metabolism of dihomo-gamma-linolenic acid and arachidonic acid by cyclo-oxygenase-1 and cyclo-oxygenase-2: implications for cellular synthesis of prostaglandin E1 and prostaglandin E2. Biochem J. 2002 Jul 15;365(Pt 2):489-96. To Reference
Ref 6Structure of eicosapentaenoic and linoleic acids in the cyclooxygenase site of prostaglandin endoperoxide H synthase-1. J Biol Chem. 2001 Oct 5;276(40):37547-55. Epub 2001 Jul 27. To Reference
Ref 7Mutational and X-ray crystallographic analysis of the interaction of dihomo-gamma -linolenic acid with prostaglandin endoperoxide H synthases. J Biol Chem. 2001 Mar 30;276(13):10358-65. Epub 2000 Dec 19. To Reference
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Professor in Department of Pharmacy
National University of Singapore, Singapore


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