From G Protein-coupled Receptor Structure Resolution to Rational Drug Design

Overview

Journal J Biol Chem

Specialty Biochemistry

Date 2015 Jun 24

PMID 26100628

Citations 37

Authors

Ali Jazayeri

Joao M Dias

Fiona H Marshall

Affiliations

Soon will be listed here.

Abstract

A number of recent technical solutions have led to significant advances in G protein-coupled receptor (GPCR) structural biology. Apart from a detailed mechanistic view of receptor activation, the new structures have revealed novel ligand binding sites. Together, these insights provide avenues for rational drug design to modulate the activities of these important drug targets. The application of structural data to GPCR drug discovery ushers in an exciting era with the potential to improve existing drugs and discover new ones. In this review, we focus on technical solutions that have accelerated GPCR crystallography as well as some of the salient findings from structures that are relevant to drug discovery. Finally, we outline some of the approaches used in GPCR structure based drug design.

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