Science Blog of Dr. Yuan分享 This blog is mainly on Molecular molecular modelling and simulations


Pharmacology: Inside-out receptor inhibition

已有 1986 次阅读 2016-12-8 16:22 |系统分类:科研笔记

Visualizing allosteric inhibition.

Structures of two chemokine receptor proteins in complex with small molecules reveal a previously unknown binding pocket that could be a drug target for treating a range of diseases involving this receptor family.

A family of cell-membrane proteins known as G-protein-coupled receptors mediates transmembrane signal transduction. One subset of this family is the chemokine receptors, which regulate cell migration and whose activation has been implicated in a range of diseases, including immune disorders and cancer. But finding drugs that inhibit these receptors has been challenging. Two papers online in Nature1, 2 now describe crystal structures of two different chemokine receptors in complex with small-molecule inhibitors. Two of these antagonists bind to pockets near to the receptors' intracellular surfaces, pointing to a previously unidentified pathway that can be targeted for drug discovery.


Intracellular allosteric antagonism of the CCR9 receptor. Oswald, al. Nature (2016).

Structure of CC chemokine receptor 2 with orthosteric and allosteric antagonists. Zheng, al. Nature (2016).

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