Therapeutic Targets Database
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TTD Target ID: TTDS00041

Target Information
NameProstaglandin G/H synthase 2    
Type of targetSuccessful target    
SynonymsCOX-2    
Cyclooxygenase -2    
Cyclooxygenase 2    
Cyclooxygenase-2    
Heme-protein prostaglandin G/H synthase    
PGH synthase 2    
PGHS-2    
PHS II    
Prostaglandin H2 synthase 2    
Prostaglandin-endoperoxide synthase 2    
DiseaseAbdominal aortic aneurysm    [1]
Adenomatous polyposis    [2]
Alzheimer's disease    [3]
Analgesics    [4][5]
Arthritis    [6]
Bladder cancer    [7]
Breast cancer    [8][9]
Cancer, unspecific    [10]
Carcinoma in situ, unspecified    [11]
Carpal tunnel syndrome    [12]
Colorectal cancer    [13][14]
Dysmenorrhea, unspecified    [15]
Endometriosis    [16]
Genitourinary tumors    [17]
Gestational hypertension    [18]
Inflammation    [19]
Inflammatory diseases    [3][20]
Lung cancer    [21]
Malignant mesothelioma    [22]
Meningioma    [23]
Myocardial infarction    [24][25]
Oropharyngeal squamous cell carcinoma    [26]
Osteoarthritis    [15]
Pain, unspecified    [4][5]
Pathological angiogenesis    [27]
Peutz-Jeghers syndrome    [28][29]
Prostate cancer    [30][31]
Pyresis    [5]
Renal cell carcinoma    [32]
Rheumatoid arthritis, unspecified    [33]
Stroke    [34]
Vascular lesion regression    [35]
Drug(s)CarprofenApprovedPain[36]
CelecoxibApprovedRheumatoid arthritis and osteoarthritis[37][38][4][15][33][15][39][2]
DiflunisalApprovedPain[40]
EtodolacApprovedPain[41][30]
EtoricoxibApprovedRheumatoid arthritis and osteoarthritis[42][43]
IbuprofenApprovedPain[44][45][5]
KetoprofenApprovedRheumatoid arthritis and pain[46]
LumiracoxibApprovedKnee osteoarthritis [47]
Mefenamic acidApprovedRheumatoid arthritis and osteoarthritis[48]
MeloxicamApprovedArthritis[49]
NabumetoneApprovedRheumatoid arthritis and osteoarthritis[50][51]
NaproxenApprovedPain and Rheumatoid arthritis[52][40]
Niflumic AcidApprovedRheumatoid arthritis[53]
PhenylbutazoneApprovedChronic pain[54]
PiroxicamApprovedPain[44][55]
TenoxicamApprovedRheumatoid arthritis and osteoarthritis[56][57]
Tiaprofenic acidApprovedPain[58]
TolmetinApprovedRheumatoid arthritis and osteoarthritis[44]
ValdecoxibApprovedOsteoarthritis and rheumatoid arthritis[59]
ONO-2506Phase III completedStroke[60]
CelecoxibPhase IIIPain[61][62][38]
GSK-644784Suspended in Phase II in GSK 2006 ReportNeuropathic pain[63]
GW-406381Suspended in Phase III in GSK 2006 ReportOsteoarthritis, Neuropathic pain[63]
RofecoxibWithdrawnOsteoarthritis[38][64][16][65][33]
NimesulidePreclinicalAcute pain; fever; osteoarthritis; dysmenorrhea[60]
RPR 200765APreclinicalRheumatoid arthritis[6]
BioChemical ClassOxidoreductases acting on paired donors    
EC NumberEC 1.14.99.1
PathwayArachidonic acid metabolism
Pathways in cancer
Small cell lung cancer
VEGF signaling pathway
UniProt IDP35354
PDB Structure1V0X.    
FunctionMay have a role as a major mediator of inflammation and/or a role for prostanoid signaling in activity-dependent plasticity.    
SequenceMLARALLLCAVLALSHTANPCCSHPCQNRGVCMSVGFDQYKCDCTRTGFYGENCSTPEFL TRIKLFLKPTPNTVHYILTHFKGFWNVVNNIPFLRNAIMSYVLTSRSHLIDSPPTYNADY GYKSWEAFSNLSYYTRALPPVPDDCPTPLGVKGKKQLPDSNEIVEKLLLRRKFIPDPQGS NMMFAFFAQHFTHQFFKTDHKRGPAFTNGLGHGVDLNHIYGETLARQRKLRLFKDGKMKY QIIDGEMYPPTVKDTQAEMIYPPQVPEHLRFAVGQEVFGLVPGLMMYATIWLREHNRVCD VLKQEHPEWGDEQLFQTSRLILIGETIKIVIEDYVQHLSGYHFKLKFDPELLFNKQFQYQ NRIAAEFNTLYHWHPLLPDTFQIHDQKYNYQQFIYNNSILLEHGITQFVESFTRQIAGRV AGGRNVPPAVQKVSQASIDQSRQMKYQSFNEYRKRFMLKPYESFEELTGEKEMSAELEAL YGDIDAVELYPALLVEKPRPDAIFGETMVEVGAPFSLKGLMGNVICSPAYWKPSTFGGEV GFQIINTASIQSLICNNVKGCPFTSFSVPDPELIKTVTINASSSRSGLDDINPTVLLKER STEL
Related US Patent6,204,387
6,252,116
6,323,226
6,340,691
6,369,275
6,376,519
6,407,140
6,432,999
6,436,967
6,440,963
6,451,794
6,465,509
6,469,040
6,472,416
6,486,194
6,486,247
6,488,734
6,492,416
6,495,517
6,512,121
6,515,014
6,534,540
6,541,646
6,555,540
6,583,321
6,589,973
6,596,736
6,599,929
6,613,790
6,617,345
6,649,629
6,649,654
6,656,968
6,670,365
6,677,364
6,768,019
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor2'-Hydroxychalcone[66]
3,4-dihydroxyxanthone[67]
B-Octylglucoside[68]
BW-755C[69]
Bimetopyrole[70]
Carprofen[36]
Celecoxib[37][38][4][15][33][15][39][2]
Celecoxib[61][62][38]
DFU[25]
Diflunisal[40]
DuP-697[5]
Etodolac[41][30]
Etoricoxib[42][43]
Firocoxib[71]
Flufenamic Acid[72]
GSK-644784[63]
GW-406381[63]
GW-637185X[73]
Heme[74]
Ibuprofen[44][45][5]
Ketoprofen[46]
L-745337[75]
L-748780[76]
L-761000[76]
LM-4108[77]
Lumiracoxib[47]
MK-886[45]
Mefenamic acid[48]
Meloxicam[49]
Microxine[78]
NS-398[13][30]
NS398[79]
NSAIDs[33]
NSC-27236[80]
Nabumetone[50][51]
Naproxen[52][40]
Naproxene[79]
Nectamazin C[81]
Niflumic Acid[53]
Nimesulide[82]
Nimesulide[60]
ONO-2506[60]
Oxametacin[83]
Phenylbutazone[54]
Piroxicam[44][55]
Prifelone[84]
Prostaglandin G2[74]
RPR 200765A[6]
RWJ-67657[85]
Resveratrol[20]
Rofecoxib[38][64][16][65][33]
SB 202190[86]
SB 203580[19]
SB 239063[87]
SC-558[88]
SC-57666[89]
SC-58125[90]
SC-58451[91]
Tenoxicam[56][57]
Tiaprofenic acid[58]
Tilmacoxib[92]
Tolmetin[44]
Valdecoxib[59]
UpRegulatorC-myb[93]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
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Ref 2The cyclooxygenase-2 inhibitor celecoxib is a potent preventive and therapeutic agent in the min mouse model of adenomatous polyposis. Cancer Res. 2000 Sep 15;60(18):5040-4. To Reference
Ref 3Cyclooxygenase (COX)-2 and cell cycle activity in a transgenic mouse model of Alzheimer's disease neuropathology. Neurobiol Aging. 2002 May-Jun;23(3):327-34. To Reference
Ref 4A randomized, clinical trial comparing oral celecoxib 200 mg, celecoxib 400 mg, and ibuprofen 600 mg for acute pain. Acad Emerg Med. 2003 Jan;10(1):22-30. To Reference
Ref 5Analysis of prostaglandin G/H synthase-2 inhibition using peroxidase-induced luminol luminescence. Anal Biochem. 1998 Nov 15;264(2):216-21. To Reference
Ref 6The discovery of RPR 200765A, a p38 MAP kinase inhibitor displaying a good oral anti-arthritic efficacy. Bioorg Med Chem. 2001 Feb;9(2):537-54. To Reference
Ref 7Enhanced expression of cyclooxygenase-2 in high grade human transitional cell bladder carcinomas. Am J Pathol. 2000 Jul;157(1):29-35. To Reference
Ref 8Cyclooxygenase-2: a potential target in breast cancer. Semin Oncol. 2004 Feb;31(1 Suppl 3):64-73. To Reference
Ref 9Cyclooxygenase-2: a target for the prevention and treatment of breast cancer. Endocr Relat Cancer. 2001 Jun;8(2):97-114. To Reference
Ref 10COX-2 inhibitors in cancer treatment and prevention, a recent development. Anticancer Drugs. 2002 Feb;13(2):127-37. To Reference
Ref 11Cyclooxygenase-2 expression is up-regulated in transitional cell carcinoma and its preneoplastic lesions in the human urinary bladder. Clin Cancer Res. 2000 Jun;6(6):2424-30. To Reference
Ref 12COX-2 up-regulation in idiopathic carpal tunnel syndrome. Plast Reconstr Surg. 2003 Dec;112(7):1807-14. To Reference
Ref 13COX-2 selective inhibition reverses the trophic properties of gastrin in colorectal cancer. Br J Cancer. 2002 Aug 27;87(5):574-9. To Reference
Ref 14Cyclooxygenase-2 expression in right- and left-sided colon cancer: a rationale for optimization of cyclooxygenase-2 inhibitor therapy. Clin Colorectal Cancer. 2004 Feb;3(4):243-7. To Reference
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Ref 30Induction of apoptosis by cyclooxygenase-2 inhibitors in prostate cancer cell lines. Int J Urol. 2001 Jul;8(7):S35-9. To Reference
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Ref 36Scaffold of the cyclooxygenase-2 (COX-2) inhibitor carprofen provides Alzheimer gamma-secretase modulators. J Med Chem. 2006 Dec 28;49(26):7588-91. To Reference
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Ref 49Variability in the response to cyclooxygenase inhibitors: toward the individualization of nonsteroidal anti-inflammatory drug therapy. J Investig Med. 2009 Aug;57(6):709-16. To Reference
Ref 50Novel determination of nabumetone, a cox-2 inhibitor precursor via its 4-carboxyl-2,6-dinitrobenzene diazonium (CDNBD) derived AZO dye. Afr J Med Med Sci. 2007 Sep;36(3):249-57. To Reference
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Ref 52Naproxcinod, a new cyclooxygenase-inhibiting nitric oxide donator (CINOD). Expert Opin Biol Ther. 2009 May;9(5):649-57. To Reference
Ref 53Rat ovulation, implantation and decidualization are severely compromised by COX-2 inhibitors. Front Biosci. 2007 May 1;12:3333-42. To Reference
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Professor in Department of Pharmacy
National University of Singapore, Singapore


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