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Curr Opin Pharmacol. 2014 Jun;16:108-15. doi: 10.1016/j.coph.2014.04.002. Epub 2014 May 14.

Biased ligands: pathway validation for novel GPCR therapeutics.

Author information

1
Trevena Inc., King of Prussia, PA, USA.
2
Trevena Inc., King of Prussia, PA, USA. Electronic address: JViolin@trevenainc.com.

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.

PMID:
24834870
DOI:
10.1016/j.coph.2014.04.002
[Indexed for MEDLINE]

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