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6COX

CYCLOOXYGENASE-2 (PROSTAGLANDIN SYNTHASE-2) COMPLEXED WITH A SELECTIVE INHIBITOR, SC-558 IN I222 SPACE GROUP

6COX の概要
エントリーDOI10.2210/pdb6cox/pdb
分子名称CYCLOOXYGENASE-2, 2-acetamido-2-deoxy-beta-D-glucopyranose, PROTOPORPHYRIN IX CONTAINING FE, ... (4 entities in total)
機能のキーワードperoxidase, dioxygenase, cyclooxygenase, nonsteroidal antiinflammatory drugs, inflammation, arthritis, prostaglandin, prostaglandin synthase, oxidoreductase
由来する生物種Mus musculus (house mouse)
タンパク質・核酸の鎖数2
化学式量合計138090.14
構造登録者
Kurumbail, R.,Stallings, W. (登録日: 1996-12-18, 公開日: 1997-12-24, 最終更新日: 2024-10-30)
主引用文献Kurumbail, R.G.,Stevens, A.M.,Gierse, J.K.,McDonald, J.J.,Stegeman, R.A.,Pak, J.Y.,Gildehaus, D.,Miyashiro, J.M.,Penning, T.D.,Seibert, K.,Isakson, P.C.,Stallings, W.C.
Structural basis for selective inhibition of cyclooxygenase-2 by anti-inflammatory agents.
Nature, 384:644-648, 1996
Cited by
PubMed Abstract: 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.
PubMed: 8967954
DOI: 10.1038/384644a0
主引用文献が同じPDBエントリー
実験手法
X-RAY DIFFRACTION (2.8 Å)
構造検証レポート
Validation report summary of 6cox
検証レポート(詳細版)ダウンロードをダウンロード

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件を2025-07-16に公開中

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