Impact of GPCR Structures on Drug Discovery

Miles Congreve; Chris de Graaf; Nigel A Swain; Christopher G Tate

doi:10.1016/j.cell.2020.03.003

Impact of GPCR Structures on Drug Discovery

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

Authors

Miles Congreve¹, Chris de Graaf¹, Nigel A Swain¹, Christopher G Tate²

Affiliations

¹ Sosei Heptares, Steinmetz Building, Granta Park, Abingdon, Cambridge CB21 6DG, UK.
² MRC Laboratory of Molecular Biology, Francis Crick Avenue, Cambridge CB2 0QH, UK. Electronic address: cgt@mrc-lmb.cam.ac.uk.

PMID: 32243800
DOI: 10.1016/j.cell.2020.03.003

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.

Publication types

Research Support, Non-U.S. Gov't
Review

MeSH terms

Drug Design*
Drug Discovery*
Humans
Ligands
Molecular Conformation
Molecular Structure
Receptors, G-Protein-Coupled / chemistry*

Substances

Ligands
Receptors, G-Protein-Coupled

Abstract

Publication types

MeSH terms

Substances

Grants and funding