2GGC

Novel bacterial methionine aminopeptidase inhibitors

2GGC の概要

• エントリーDOI: 10.2210/pdb2ggc/pdb
• 関連するPDBエントリー: 2GG0 2GG2 2GG3 2GG5 2GG7 2GG8 2GG9 2GGB
• 分子名称: Methionine aminopeptidase, COBALT (II) ION, SODIUM ION, ... (5 entities in total)
• 機能のキーワード: methionine amino peptidase, pita-bread fold, map inhibitor, antibacterial, hydrolase
• 由来する生物種: Escherichia coli K12
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 29529.71

構造登録者

Evdokimov, A.G.,Pokross, M.E.,Walter, R.L.,Mekel, M. (登録日: 2006-03-23, 公開日: 2006-06-13, 最終更新日: 2023-08-30)

主引用文献

Evdokimov, A.G.,Pokross, M.,Walter, R.L.,Mekel, M.,Barnett, B.L.,Amburgey, J.,Seibel, W.L.,Soper, S.J.,Djung, J.F.,Fairweather, N.,Diven, C.,Rastogi, V.,Grinius, L.,Klanke, C.,Siehnel, R.,Twinem, T.,Andrews, R.,Curnow, A.
Serendipitous discovery of novel bacterial methionine aminopeptidase inhibitors.
Proteins, 66:538-546, 2007

PubMed Abstract: In this article we describe the application of structural biology methods to the discovery of novel potent inhibitors of methionine aminopeptidases. These enzymes are employed by the cells to cleave the N-terminal methionine from nascent peptides and proteins. As this is one of the critical steps in protein maturation, it is very likely that inhibitors of these enzymes may prove useful as novel antibacterial agents. Involvement of crystallography at the very early stages of the inhibitor design process resulted in serendipitous discovery of a new inhibitor class, the pyrazole-diamines. Atomic-resolution structures of several inhibitors bound to the enzyme illuminate a new mode of inhibitor binding.

PubMed: 17120228
DOI: 10.1002/prot.21207

実験手法

X-RAY DIFFRACTION (1 Å)