Structures of mGluRs shed light on the challenges of drug development of allosteric modulators.

Kirstie A Bennett,Andrew S Doré,John A Christopher,Dahlia R Weiss,Fiona H Marshall

Current Opinion in Pharmacology（2015）

引用 29|浏览8

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摘要

•X-ray structures of the transmembrane domains of mGlu1 and mGlu5 have been solved.•These explain the difficulties encountered in developing allosteric modulator drugs.•The mechanisms underlying mGlu5 pharmacological mode switching are revealed.•Structure based approaches to drug discovery can now be applied to class C GPCRs.

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