2GA2

h-MetAP2 complexed with A193400

2GA2 の概要

• エントリーDOI: 10.2210/pdb2ga2/pdb
• 分子名称: Methionine aminopeptidase 2, MANGANESE (II) ION, 5-BROMO-2-{[(4-CHLOROPHENYL)SULFONYL]AMINO}BENZOIC ACID, ... (4 entities in total)
• 機能のキーワード: complex, hydrolase
• 由来する生物種: Homo sapiens (human)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 41870.52

構造登録者

Park, C. (登録日: 2006-03-07, 公開日: 2007-03-13, 最終更新日: 2024-10-30)

主引用文献

Kawai, M.,BaMaung, N.Y.,Fidanze, S.D.,Erickson, S.A.,Tedrow, J.S.,Sanders, W.J.,Vasudevan, A.,Park, C.,Hutchins, C.,Comess, K.M.,Kalvin, D.,Wang, J.,Zhang, Q.,Lou, P.,Tucker-Garcia, L.,Bouska, J.,Bell, R.L.,Lesniewski, R.,Henkin, J.,Sheppard, G.S.
Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties.
Bioorg.Med.Chem.Lett., 16:3574-3577, 2006

PubMed Abstract: We have screened molecules for inhibition of MetAP2 as a novel approach toward antiangiogenesis and anticancer therapy using affinity selection/mass spectrometry (ASMS) employing MetAP2 loaded with Mn(2+) as the active site metal. After a series of anthranilic acid sulfonamides with micromolar affinities was identified, chemistry efforts were initiated. The micromolar hits were quickly improved to potent nanomolar inhibitors by chemical modifications guided by insights from X-ray crystallography.

PubMed: 16632353
DOI: 10.1016/j.bmcl.2006.03.085

実験手法

X-RAY DIFFRACTION (1.95 Å)