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2BB7

Mn Form Of E. coli Methionine Aminopeptidase In Complex With a quinolinyl sulfonamide inhibitor

2BB7 の概要
エントリーDOI10.2210/pdb2bb7/pdb
分子名称Methionine aminopeptidase, MANGANESE (II) ION, SODIUM ION, ... (5 entities in total)
機能のキーワードtrimetallic, mn(ii)-form, hydrolase, enzyme-inhibitor complex, metalloenzyme
由来する生物種Escherichia coli
タンパク質・核酸の鎖数1
化学式量合計29780.91
構造登録者
Ye, Q.Z. (登録日: 2005-10-17, 公開日: 2006-01-24, 最終更新日: 2023-08-23)
主引用文献Huang, M.,Xie, S.X.,Ma, Z.Q.,Hanzlik, R.P.,Ye, Q.Z.
Metal mediated inhibition of methionine aminopeptidase by quinolinyl sulfonamides
Biochem.Biophys.Res.Commun., 339:506-513, 2006
Cited by
PubMed Abstract: Quinolinyl sulfonamides, such as N-(quinolin-8-yl)methanesulfonamide (10) and N-(5-chloroquinolin-8-yl)methanesulfonamide (11), were identified as potent methionine aminopeptidase (MetAP) inhibitors by high throughput screening of a diverse chemical library of small organic compounds. They showed different inhibitory potencies on Co(II)-, Ni(II)-, Fe(II)-, Mn(II)-, and Zn(II)-forms of Escherichia coli MetAP, and their inhibition is dependent on metal concentration. X-ray structures of E. coli MetAP complexed with 10 revealed that the inhibitor forms a metal complex with the residue H79 at the enzyme active site; the complex is further stabilized by an extended H-bond and metal interaction network. Analysis of the inhibition of MetAP by these inhibitors indicates that this is a typical mechanism of inhibition for many non-peptidic MetAP inhibitors and emphasizes the importance of defining in vitro conditions for identifying and evaluating MetAP inhibitors that will be capable of giving information relevant to the in vivo situation.
PubMed: 16300729
DOI: 10.1016/j.bbrc.2005.11.042
主引用文献が同じPDBエントリー
実験手法
X-RAY DIFFRACTION (1.7 Å)
構造検証レポート
Validation report summary of 2bb7
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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