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

文献索引：FEBS Lett. 587(22) , 3681-6, (2013)

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摘要

• 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.