Cyclooxygenase

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NSAIDs

Table X: Selectivity of some NSAIDs

Drug	Coefficient of selectivity (IC50Cox-1/IC50Cox-2)
Ketorolac	100-1000
Naproxen	1-10
Ibuprofen	1-10
Indometacin	1-10
Acetylsalicylic acid	1
Diclofenac	1-0.1
Valdecoxib	0.01-0.001
Etoricoxib	0.01-0.001

Table X: Chemical variety of NSAIDs

Pharmacologic group	Drug
Salicylates	Acetylsalicylic acid
Propionic	Naproxen
	Ibuprofen
Para-aminophenols	Paracetamol
Indolacetic	Indometacin
Pirrolacetic	Ketorolac
Phenilacetic	Diclofenac
Piranoidacetic	Etodolac
Anthranilic	Mefenamic acid
Nicotinic	Clonixin
Sulfonanilides	Nimesulide

Reference

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• Smith WL, DeWitt DL, Garavito RM. Cyclooxygenases: structural, cellular, and molecular biology. Annu Rev Biochem. 2000;69:145-82. PMID:10966456 doi:10.1146/annurev.biochem.69.1.145

• Rang HP, Dale MM, Ritter JM, Flower RJ. 2008. Pharmacology. Elsevier. 6th edition. 844 p.

• Smith WL, Langenbach R. Why there are two cyclooxygenase isozymes. J Clin Invest. 2001 Jun;107(12):1491-5. PMID:11413152 doi:10.1172/JCI13271

• Chandrasekharan NV, Dai H, Roos KL, Evanson NK, Tomsik J, Elton TS, Simmons DL. 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. PMID:12242329 doi:10.1073/pnas.162468699

• Garavito RM, Mulichak AM. The structure of mammalian cyclooxygenases. Annu Rev Biophys Biomol Struct. 2003;32:183-206. Epub 2003 Feb 5. PMID:12574066 doi:10.1146/annurev.biophys.32.110601.141906

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• Spencer AG, Thuresson E, Otto JC, Song I, Smith T, DeWitt DL, Garavito RM, Smith WL. The membrane binding domains of prostaglandin endoperoxide H synthases 1 and 2. Peptide mapping and mutational analysis. J Biol Chem. 1999 Nov 12;274(46):32936-42. PMID:10551860

• Luong C, Miller A, Barnett J, Chow J, Ramesha C, Browner MF. Flexibility of the NSAID binding site in the structure of human cyclooxygenase-2. Nat Struct Biol. 1996 Nov;3(11):927-33. PMID:8901870

• Kurumbail RG, Stevens AM, Gierse JK, McDonald JJ, Stegeman RA, Pak JY, Gildehaus D, Miyashiro JM, Penning TD, Seibert K, Isakson PC, Stallings WC. Structural basis for selective inhibition of cyclooxygenase-2 by anti-inflammatory agents. Nature. 1996 Dec 19-26;384(6610):644-8. PMID:8967954 doi:http://dx.doi.org/10.1038/384644a0