View source for 5cox

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'''UNINHIBITED MOUSE CYCLOOXYGENASE-2 (PROSTAGLANDIN SYNTHASE-2)'''<br />

==Overview==
Prostaglandins and glucocorticoids are potent mediators of inflammation., Non-steroidal anti-inflammatory drugs (NSAIDs) exert their effects by, inhibition of prostaglandin production. The pharmacological target of, NSAIDs is cyclooxygenase (COX, also known as PGH synthase), which, catalyses the first committed step in arachidonic-acid metabolism. Two, isoforms of the membrane protein COX are known: COX-1, which is, constitutively expressed in most tissues, is responsible for the, physiological production of prostaglandins; and COX-2, which is induced by, cytokines, mitogens and endotoxins in inflammatory cells, is responsible, for the elevated production of prostaglandins during inflammation. The, structure of ovine COX-1 complexed with several NSAIDs has been, determined. Here we report the structures of unliganded murine COX-2 and, complexes with flurbiprofen, indomethacin and SC-558, a selective COX-2, inhibitor, determined at 3.0 to 2.5 A resolution. These structures explain, the structural basis for the selective inhibition of COX-2, and, demonstrate some of the conformational changes associated with, time-dependent inhibition.

==About this Structure==
5COX is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus] with NAG and HEM as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Prostaglandin-endoperoxide_synthase Prostaglandin-endoperoxide synthase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.14.99.1 1.14.99.1] Known structural/functional Sites: <scene name='pdbsite=ACE:SER 530 Is Acetylated By Aspirin (An Acetyl Group Is Cov ...'>ACE</scene>, <scene name='pdbsite=CAT:TYR 385 Is Believed To Be The Amino Acid That Abstracts ...'>CAT</scene>, <scene name='pdbsite=HEM:HIS 388 Is The Axial Ligand To The Heme'>HEM</scene> and <scene name='pdbsite=SUB:ARG 120 Is Believed To Anchor The Carboxylate Of Substra ...'>SUB</scene>. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=5COX OCA]. 

==Reference==
Structural basis for selective inhibition of cyclooxygenase-2 by anti-inflammatory agents., Kurumbail RG, Stevens AM, Gierse JK, McDonald JJ, Stegeman RA, Pak JY, Gildehaus D, Miyashiro JM, Penning TD, Seibert K, Isakson PC, Stallings WC, Nature. 1996 Dec 19-26;384(6610):644-8. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=8967954 8967954]
[[Category: Mus musculus]]
[[Category: Prostaglandin-endoperoxide synthase]]
[[Category: Single protein]]
[[Category: Kurumbail, R.]]
[[Category: Stallings, W.]]
[[Category: HEM]]
[[Category: NAG]]
[[Category: arthritis]]
[[Category: cyclooxygenase]]
[[Category: dioxygenase]]
[[Category: inflammation]]
[[Category: nonsteroidal antiinflammatory drugs]]
[[Category: oxidoreductase]]
[[Category: peroxidase]]
[[Category: prostaglandin]]
[[Category: prostaglandin synthase]]

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