Biased ligands: pathway validation for novel GPCR therapeutics.

Abstract:

:G protein-coupled receptors (GPCRs), in recent years, have been shown to signal via multiple distinct pathways. Furthermore, biased ligands for some receptors can differentially stimulate or inhibit these pathways versus unbiased endogenous ligands or drugs. Biased ligands can be used to gain a deeper understanding of the molecular targets and cellular responses associated with a GPCR, and may be developed into therapeutics with improved efficacy, safety and/or tolerability. Here we review examples and approaches to pathway validation that establish the relevance and therapeutic potential of distinct pathways that can be selectively activated or blocked by biased ligands.

journal_name

Curr Opin Pharmacol

authors

Rominger DH,Cowan CL,Gowen-MacDonald W,Violin JD

doi

10.1016/j.coph.2014.04.002

subject

Has Abstract

pub_date

2014-06-01 00:00:00

pages

108-15

eissn

1471-4892

issn

1471-4973

pii

S1471-4892(14)00041-1

journal_volume

16

pub_type

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