TTD Target ID: TTDS00039

Target Information
Name	Cyclooxygenase
Type of target	Successful target
Synonyms	Cyclooxygenase (COX1 and COX2)
	PHS
	Prostaglandin H2 synthase
	Prostaglandin synthase
Disease	Cardiovascular disease, unspecified [ICD9: 390-459   ICD10: I00-I99]				[1][2]
	Inflammatory diseases				[3]
Drug(s)	Acetaminophen		Approved	Pain	[4][5][6]
	Aspirin		Approved	Pain	[7]
	Diclofenac		Approved	Rheumatoid arthritis	[8][9]
	Fenoprofen		Approved	Rheumatoid arthritis	[10][11]
	Flurbiprofen		Approved	Rheumatoid arthritis	[12]
	Fosfosal		Approved	Analgesic	[13][14]
	Icosapent		Approved	Hyperglyceridemic	[15]
	Indomethacin		Approved	Patent ductus arteriosus	[16]
	Ketorolac		Approved	Pain	[17]
	Meclofenamic acid		Approved	Joint and muscular pain	[18][19]
	Oxaprozin		Approved	Inflammatory diseases	[10]
	Sulindac sulfide		Approved	Rheumatoid arthritis	[20]
	Asasantin		Marketed	Cerebrovascular ischaemia	[21]
	Pravigard		Marketed	Myocardial infarction, cerebrovascular ischaemia	[21]
	Benzydamine		Phase II terminated	Chemotherapy- or radiotherapy-induced mucositis, pain relief	[22]
	NCX-4016		Terminated in Phase II	Type 2 Diabetes, Early Nephropathy, Claudication, inflammation, pain, vein graft restenosis, thrombosis	[21]
BioChemical Class	Oxidoreductases acting on paired donors
Pathway	Arachidonic acid metabolism
	Metabolic pathways
Target Validation	Click to Find Target Validation Information.
QSAR Model	Click to Find Target QSAR Model.
Inhibitor	Acetaminophen		[4][5][6]
	Asasantin		[21]
	Aspirin		[7]
	BN82451		[23]
	Benzydamine		[22]
	Diclofenac		[8][9]
	Fenoprofen		[10][11]
	Flurbiprofen		[12]
	Indomethacin		[16]
	Ketorolac		[17]
	Meclofenamate		[18][19]
	Meclofenamic acid		[18][19]
	NCX-4016		[21]
	Oxaprozin		[10]
	Pravigard		[21]
	Sulindac sulfide		[20]
Binder	Icosapent		[15]
Multitarget	Pravigard		[21]
Cross References	3D Structure Related Literature On-Line Medical Dictionary
Ref 1	Prostaglandin synthase. At the heart of the matter. Curr Biol. 1994 May 1;4(5):452-4. To Reference
Ref 2	Prostaglandin H synthases, nonsteroidal anti-inflammatory drugs, and colon cancer. FASEB J. 1997 Mar;11(4):234-47. To Reference
Ref 3	The 2.0 A resolution crystal structure of prostaglandin H2 synthase-1: structural insights into an unusual peroxidase. J Mol Biol. 2004 Jan 9;335(2):503-18. To Reference
Ref 4	Mechanism of action of paracetamol. Am J Ther. 2005 Jan-Feb;12(1):46-55. To Reference
Ref 5	COX-3: just another COX or the solitary elusive target of paracetamol? Lancet. 2003 Mar 22;361(9362):981-2. To Reference
Ref 6	COX-3, a cyclooxygenase-1 variant inhibited by acetaminophen and other analgesic/antipyretic drugs: cloning, structure, and expression. Proc Natl Acad Sci U S A. 2002 Oct 15;99(21):13926-31. Epub 2002 Sep 19. To Reference
Ref 7	Cyclooxygenase inhibitors: instrumental drugs to understand cardiovascular homeostasis and arterial thrombosis. Cardiovasc Hematol Disord Drug Targets. 2008 Dec;8(4):268-77. To Reference
Ref 8	Aqueous extract of Asiasari radix inhibits formalin-induced hyperalgesia via NMDA receptors. J Ethnopharmacol. 2009 May 4;123(1):128-33. Epub 2009 Feb 14. To Reference
Ref 9	Nat Rev Drug Discov. 2003 Jan;2(1):38-51.Knockouts model the 100 best-selling drugs--will they model the next 100? To Reference
Ref 10	The aryl propionic acid R-flurbiprofen selectively induces p75NTR-dependent decreased survival of prostate tumor cells. Cancer Res. 2007 Apr 1;67(7):3254-62. To Reference
Ref 11	Immunomodulatory effect of nonsteroidal anti-inflammatory drugs (NSAIDs) at the clinically available doses. Arch Pharm Res. 2007 Jan;30(1):64-74. To Reference
Ref 12	In vitro and in vivo profiling of CHF5022 and CHF5074 Two beta-amyloid1-42 lowering agents. Pharmacol Res. 2007 Apr;55(4):318-28. Epub 2007 Jan 16. To Reference
Ref 13	Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20. To Reference
Ref 14	6251858 To Reference
Ref 15	Differential modulation of Toll-like receptors by fatty acids: preferential inhibition by n-3 polyunsaturated fatty acids. J Lipid Res. 2003 Mar;44(3):479-86. Epub 2002 Dec 1. To Reference
Ref 16	Indomethacin decreases arachidonic acid uptake in HCA-7 human colon cancer cells. J Pharmacol Sci. 2008 Nov;108(3):389-92. Epub 2008 Nov 6. To Reference
Ref 17	Cyclooxygenase and nitric oxide synthase dependence of cutaneous reactive hyperemia in humans. Am J Physiol Heart Circ Physiol. 2007 Jul;293(1):H425-32. Epub 2007 Mar 16. To Reference
Ref 18	Interactions of PGH synthase isozymes-1 and -2 with NSAIDs. Ann N Y Acad Sci. 1994 Nov 15;744:50-7. To Reference
Ref 19	Pharmacology of prostaglandin endoperoxide synthase isozymes-1 and -2. Ann N Y Acad Sci. 1994 Apr 18;714:136-42. To Reference
Ref 20	A novel sulindac derivative that does not inhibit cyclooxygenases but potently inhibits colon tumor cell growth and induces apoptosis with antitumor activity. Cancer Prev Res (Phila Pa). 2009 Jun;2(6):572-80. Epub 2009 May 26. To Reference
Ref 21	Emerging drugs in peripheral arterial disease. Expert Opin Emerg Drugs. 2006 Mar;11(1):75-90. To Reference
Ref 22	Emerging drugs for chemotherapy-induced mucositis. Expert Opin Emerg Drugs. 2008 Sep;13(3):511-22. To Reference
Ref 23	Emerging drug therapies in Huntington's disease. Expert Opin Emerg Drugs. 2009 Jun;14(2):273-97. To Reference

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