Conformational Transitions and the Activation of Heterotrimeric G Proteins by G Protein-Coupled Receptors

Christopher Draper-Joyce, Sebastian George Barton Furness

Research output: Contribution to journalArticleResearchpeer-review

Abstract

G protein-coupled receptors (GPCRs) are particularly attractive targets for therapeutic pharmaceuticals. This is because they are involved in almost all facets of physiology, in many pathophysiological processes, they are tractable due to their cell surface location, and can exhibit highly textured pharmacology. While the development of new drugs does not require the molecular details of the mechanism of activity for a particular target, there has been increasing interest in the GPCR field in these details. In part, this has come with the recognition that differential activity at a particular target might be a way in which to leverage drug activity, either through manipulation of efficacy or through differential coupling (signaling bias). To this end, the past few years have seen a number of publications that have specifically attempted to address one or more aspects of the molecular reaction pathway, leading to activation of heterotrimeric G proteins by GPCRs.
Original languageEnglish
Pages (from-to)285-290
Number of pages6
JournalACS Pharmacology & Translational Science
Volume2
Issue number4
DOIs
Publication statusPublished - 26 Jul 2019

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