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Molecular targeting of G? and G?? subunits: a potential approach for cancer therapeutics.

ABSTRACT: G-Protein-coupled receptors (GPCRs) signal through G protein ? and ?? subunit families to regulate a wide range of physiological and pathophysiological processes. As such, GPCRs are major targets for therapeutic drugs. Downstream targets of GPCRs have also gained interest as a therapeutic approach to complex pathologies involving multiple GPCRs. One such approach involves targeting of the G proteins themselves. Several small molecule G? and G?? modulators have been developed and been tested in various animal models of disease. Here we will discuss the requirements for targeting G? and G?? subunits, the mechanisms of action of currently identified inhibitors, and focus on the potential utility of G? and G?? inhibitors in the treatment of various cancers.

SUBMITTER: Smrcka AV

PROVIDER: S-EPMC3924570 | biostudies-literature | 2013 May

REPOSITORIES: biostudies-literature

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Molecular targeting of Gα and Gβγ subunits: a potential approach for cancer therapeutics.

Smrcka Alan V AV

Trends in pharmacological sciences 20130401 5

G-Protein-coupled receptors (GPCRs) signal through G protein α and βγ subunit families to regulate a wide range of physiological and pathophysiological processes. As such, GPCRs are major targets for therapeutic drugs. Downstream targets of GPCRs have also gained interest as a therapeutic approach to complex pathologies involving multiple GPCRs. One such approach involves targeting of the G proteins themselves. Several small molecule Gα and Gβγ modulators have been developed and been tested in v ...[more]

PMID: 23557963

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