Impact of GPCR Structures on Drug Discovery.

Congreve, Miles; de Graaf, Chris; Swain, Nigel A; Tate, Christopher G · Cell · 2020

review · Level V

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Abstract

Structures of 70 unique G protein-coupled receptors (GPCRs) have been determined, with over 370 structures in total bound to different ligands and the receptors in various conformational states. Structure-based drug design has been applied to an increasing number of GPCR targets over the past decade and now a few of these drug candidates have entered clinical trials. Given the length of time required for a drug to reach the market, there are no documented examples of licensed drugs being developed with the aid of a structure, but this is likely to change as current efforts come to fruition.

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