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Contribution of heteromerization to G protein-coupled receptor function.

ABSTRACT: G protein-coupled receptors (GPCRs) are a remarkably multifaceted family of transmembrane proteins that exert a variety of physiological effects. Although family A GPCRs are able to operate as monomers, there is increasing evidence that heteromerization represents a fundamental aspect of receptor function, trafficking and pharmacology. Most recently, it has been suggested that GPCR heteromers may play a crucial role as new molecular targets of heteromer-selective and bivalent ligands. The current review summarizes key recent developments in these topics.

SUBMITTER: Gaitonde SA

PROVIDER: S-EPMC5395348 | biostudies-literature | 2017 Feb

REPOSITORIES: biostudies-literature

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Contribution of heteromerization to G protein-coupled receptor function.

Gaitonde Supriya A SA González-Maeso Javier J

Current opinion in pharmacology 20161109

G protein-coupled receptors (GPCRs) are a remarkably multifaceted family of transmembrane proteins that exert a variety of physiological effects. Although family A GPCRs are able to operate as monomers, there is increasing evidence that heteromerization represents a fundamental aspect of receptor function, trafficking and pharmacology. Most recently, it has been suggested that GPCR heteromers may play a crucial role as new molecular targets of heteromer-selective and bivalent ligands. The curren ...[more]

PMID: 27835800

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