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Inhibitor selectivity between aldo–keto reductase superfamily members AKR1B10 and AKR1B1: Role of Trp112 (Trp111).

Authors :
Zhang, Liping
Zhang, Hong
Zhao, Yining
Li, Zhe
Chen, Shangke
Zhai, Jing
Chen, Yunyun
Xie, Wei
Wang, Zhong
Li, Qing
Zheng, Xuehua
Hu, Xiaopeng
Source :
FEBS Letters. Nov2013, Vol. 587 Issue 22, p3681-3686. 6p.
Publication Year :
2013

Abstract

Highlights: [•] Crystal structures of AKR1B10 holoenzyme. [•] Trp112 side-chain flipping in AKR1B10 explains non-selectivity of AKR1B1 inhibitors. [•] Native Trp112 side-chain orientation is critical for selective AKR1B10 inhibitors. [Copyright &y& Elsevier]

Details

Language :
English
ISSN :
00145793
Volume :
587
Issue :
22
Database :
Academic Search Index
Journal :
FEBS Letters
Publication Type :
Academic Journal
Accession number :
91848661
Full Text :
https://doi.org/10.1016/j.febslet.2013.09.031