Article
Molecular basis defining the selectivity of substituted isoquinolinones for the melatonin MT2 receptor.
Biochemical pharmacology - 1 Jul 2020
Chan King H, Tse Lap H, Huang Xuhui, Wong Yung H
Abstract excerpt
Melatonin MT1 and MT2 receptors represent attractive drug targets for the treatment of various disorders. However, the high conservation of the melatonin binding pocket has hindered the development of subtype-selective compounds. By leveraging on the recently resolved crystal structures of MT1 and MT2 receptors, this study aims to elucidate the structural basis of MT2-selectivity of a panel of isoquinolinone...
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