Tuning up the right signal: chemical and genetic approaches to study GPCR functions.

Abstract:

:The G protein-coupled receptor (GPCR) family is among the most druggable families in the human proteome. GPCRs are involved in most physiological processes, and our ability to modulate their activity is a hallmark of modern pharmacology. The means by which the activity of GPCRs can be modulated have been expanded by emerging data and concepts in pharmacology, which has created new strategies for their control. These new approaches will lead to the generation of more potent, selective, and efficient pharmaceutics, while reducing inappropriate actions and adverse effects. Herein, we review and comment on some recent advances in chemical and genetic approaches to the profiling of GPCR function, as well as the validation of orphan GPCRs as potential therapeutic targets using engineered receptors.

journal_name

Curr Opin Cell Biol

authors

Giguere PM,Kroeze WK,Roth BL

doi

10.1016/j.ceb.2013.11.006

subject

Has Abstract

pub_date

2014-04-01 00:00:00

pages

51-5

eissn

0955-0674

issn

1879-0410

pii

S0955-0674(13)00182-8

journal_volume

27

pub_type

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