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Review
. 2020 Apr 2;181(1):81-91.
doi: 10.1016/j.cell.2020.03.003.

Impact of GPCR Structures on Drug Discovery

Miles Congreve  1 , Chris de Graaf  1 , Nigel A Swain  1 , Christopher G Tate  2
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Free article
Review

Impact of GPCR Structures on Drug Discovery

Miles Congreve et al. Cell. .
Free article

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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Conflict of interest statement

Declarations of Interest C.G.T. is a founder of Heptares Therapeutics and is a shareholder, scientific advisory board member, and consultant for Sosei Heptares. M.C., N.A.S., and C.d.G. are employees of Heptares Therapeutics and are shareholders of Sosei Heptares.

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