2QVE

Crystal Structure of SgTAM bound to mechanism based inhibitor

2QVE の概要

• エントリーDOI: 10.2210/pdb2qve/pdb
• 関連するPDBエントリー: 2OHY
• 分子名称: Tyrosine Aminomutase, (3R)-3-amino-2,2-difluoro-3-(4-hydroxyphenyl)propanoic acid (3 entities in total)
• 機能のキーワード: mio, aminomutase, enediyne, transferase
• 由来する生物種: Streptomyces globisporus
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 114341.02

構造登録者

Christianson, C.V.,Montavon, T.J.,Bruner, S.D. (登録日: 2007-08-08, 公開日: 2008-07-22, 最終更新日: 2023-11-15)

主引用文献

Montavon, T.J.,Christianson, C.V.,Festin, G.M.,Shen, B.,Bruner, S.D.
Design and characterization of mechanism-based inhibitors for the tyrosine aminomutase SgTAM
Bioorg.Med.Chem.Lett., 18:3099-3102, 2008

PubMed Abstract: The synthesis and evaluation of two classes of inhibitors for SgTAM, a 4-methylideneimidazole-5-one (MIO) containing tyrosine aminomutase, are described. A mechanism-based strategy was used to design analogs that mimic the substrate or product of the reaction and form covalent interactions with the enzyme through the MIO prosthetic group. The analogs were characterized by measuring inhibition constants and X-ray crystallographic structural analysis of the co-complexes bound to the aminomutase, SgTAM.

PubMed: 18078753
DOI: 10.1016/j.bmcl.2007.11.046

実験手法

X-RAY DIFFRACTION (2 Å)