Detailed Information (TTD) -- BIDD

TTD Target ID: TTDS00041

Target Information
Name	Prostaglandin G/H synthase 2
Type of target	Successful target
Synonyms	COX-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
Disease	Abdominal 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)	Carprofen	Approved	Pain	[36]
	Celecoxib	Approved	Rheumatoid arthritis and osteoarthritis	[37][38][4][15][33][15][39][2]
	Diflunisal	Approved	Pain	[40]
	Etodolac	Approved	Pain	[41][30]
	Etoricoxib	Approved	Rheumatoid arthritis and osteoarthritis	[42][43]
	Ibuprofen	Approved	Pain	[44][45][5]
	Ketoprofen	Approved	Rheumatoid arthritis and pain	[46]
	Lumiracoxib	Approved	Knee osteoarthritis	[47]
	Mefenamic acid	Approved	Rheumatoid arthritis and osteoarthritis	[48]
	Meloxicam	Approved	Arthritis	[49]
	Nabumetone	Approved	Rheumatoid arthritis and osteoarthritis	[50][51]
	Naproxen	Approved	Pain and Rheumatoid arthritis	[52][40]
	Niflumic Acid	Approved	Rheumatoid arthritis	[53]
	Phenylbutazone	Approved	Chronic pain	[54]
	Piroxicam	Approved	Pain	[44][55]
	Tenoxicam	Approved	Rheumatoid arthritis and osteoarthritis	[56][57]
	Tiaprofenic acid	Approved	Pain	[58]
	Tolmetin	Approved	Rheumatoid arthritis and osteoarthritis	[44]
	Valdecoxib	Approved	Osteoarthritis and rheumatoid arthritis	[59]
	ONO-2506	Phase III completed	Stroke	[60]
	Celecoxib	Phase III	Pain	[61][62][38]
	GSK-644784	Suspended in Phase II in GSK 2006 Report	Neuropathic pain	[63]
	GW-406381	Suspended in Phase III in GSK 2006 Report	Osteoarthritis, Neuropathic pain	[63]
	Rofecoxib	Withdrawn	Osteoarthritis	[38][64][16][65][33]
	Nimesulide	Preclinical	Acute pain; fever; osteoarthritis; dysmenorrhea	[60]
	RPR 200765A	Preclinical	Rheumatoid arthritis	[6]
BioChemical Class	Oxidoreductases acting on paired donors
EC Number	EC 1.14.99.1
Pathway	Arachidonic acid metabolism
	Pathways in cancer
	Small cell lung cancer
	VEGF signaling pathway
UniProt ID	P35354
PDB Structure	1V0X.
Function	May have a role as a major mediator of inflammation and/or a role for prostanoid signaling in activity-dependent plasticity.
Sequence	MLARALLLCAVLALSHTANPCCSHPCQNRGVCMSVGFDQYKCDCTRTGFYGENCSTPEFL TRIKLFLKPTPNTVHYILTHFKGFWNVVNNIPFLRNAIMSYVLTSRSHLIDSPPTYNADY GYKSWEAFSNLSYYTRALPPVPDDCPTPLGVKGKKQLPDSNEIVEKLLLRRKFIPDPQGS NMMFAFFAQHFTHQFFKTDHKRGPAFTNGLGHGVDLNHIYGETLARQRKLRLFKDGKMKY QIIDGEMYPPTVKDTQAEMIYPPQVPEHLRFAVGQEVFGLVPGLMMYATIWLREHNRVCD VLKQEHPEWGDEQLFQTSRLILIGETIKIVIEDYVQHLSGYHFKLKFDPELLFNKQFQYQ NRIAAEFNTLYHWHPLLPDTFQIHDQKYNYQQFIYNNSILLEHGITQFVESFTRQIAGRV AGGRNVPPAVQKVSQASIDQSRQMKYQSFNEYRKRFMLKPYESFEELTGEKEMSAELEAL YGDIDAVELYPALLVEKPRPDAIFGETMVEVGAPFSLKGLMGNVICSPAYWKPSTFGGEV GFQIINTASIQSLICNNVKGCPFTSFSVPDPELIKTVTINASSSRSGLDDINPTVLLKER STEL
Related US Patent	6,204,387
	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 Validation	Click to Find Target Validation Information.
QSAR Model	Click to Find Target QSAR Model.
Inhibitor	2'-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]
UpRegulator	C-myb	[93]
Cross References	3D Structure Related Literature On-Line Medical Dictionary
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Ref 3	Cyclooxygenase (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 4	A 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 5	Analysis of prostaglandin G/H synthase-2 inhibition using peroxidase-induced luminol luminescence. Anal Biochem. 1998 Nov 15;264(2):216-21. To Reference
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