FEBS Letters 2013-11-15

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

Liping Zhang, Hong Zhang, Yining Zhao, Zhe Li, Shangke Chen, Jing Zhai, Yunyun Chen, Wei Xie, Zhong Wang, Qing Li, Xuehua Zheng, Xiaopeng Hu

Index: FEBS Lett. 587(22) , 3681-6, (2013)

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Abstract

• 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.