3pgh
From Proteopedia
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| - | [[Image:3pgh.gif|left|200px]] | + | [[Image:3pgh.gif|left|200px]] |
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| - | '''CYCLOOXYGENASE-2 (PROSTAGLANDIN SYNTHASE-2) COMPLEXED WITH A NON-SELECTIVE INHIBITOR, FLURBIPROFEN''' | + | {{Structure |
| + | |PDB= 3pgh |SIZE=350|CAPTION= <scene name='initialview01'>3pgh</scene>, resolution 2.5Å | ||
| + | |SITE= <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> | ||
| + | |LIGAND= <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=HEM:PROTOPORPHYRIN+IX+CONTAINING+FE'>HEM</scene> and <scene name='pdbligand=FLP:FLURBIPROFEN'>FLP</scene> | ||
| + | |ACTIVITY= [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] | ||
| + | |GENE= | ||
| + | }} | ||
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| + | '''CYCLOOXYGENASE-2 (PROSTAGLANDIN SYNTHASE-2) COMPLEXED WITH A NON-SELECTIVE INHIBITOR, FLURBIPROFEN''' | ||
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==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 3PGH is a [ | + | 3PGH is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3PGH OCA]. |
==Reference== | ==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:// | + | 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://www.ncbi.nlm.nih.gov/pubmed/8967954 8967954] |
[[Category: Mus musculus]] | [[Category: Mus musculus]] | ||
[[Category: Prostaglandin-endoperoxide synthase]] | [[Category: Prostaglandin-endoperoxide synthase]] | ||
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[[Category: dioxygenase]] | [[Category: dioxygenase]] | ||
[[Category: inflammation]] | [[Category: inflammation]] | ||
| - | [[Category: nonsteroidal antiinflammatory | + | [[Category: nonsteroidal antiinflammatory drug]] |
[[Category: oxidoreductase]] | [[Category: oxidoreductase]] | ||
[[Category: peroxidase]] | [[Category: peroxidase]] | ||
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[[Category: prostaglandin synthase]] | [[Category: prostaglandin synthase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 19:06:34 2008'' |
Revision as of 17:06, 20 March 2008
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| , resolution 2.5Å | |||||||
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| Sites: | , , and | ||||||
| Ligands: | , and | ||||||
| Activity: | Prostaglandin-endoperoxide synthase, with EC number 1.14.99.1 | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
CYCLOOXYGENASE-2 (PROSTAGLANDIN SYNTHASE-2) COMPLEXED WITH A NON-SELECTIVE INHIBITOR, FLURBIPROFEN
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
3PGH is a Single protein structure of sequence from Mus musculus. Full crystallographic information is available from 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:8967954
Page seeded by OCA on Thu Mar 20 19:06:34 2008
