Impact of GPCR Structures on Drug Discovery

Overview

Journal Cell

Publisher Cell Press

Specialty Cell Biology

Date 2020 Apr 4

PMID 32243800

Citations 150

Authors

Miles Congreve

Chris de Graaf

Nigel A Swain

Christopher G Tate

Affiliations

Soon will be listed here.

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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