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Rapid CommunicationMinireviews

Activators of G Protein Signaling Exhibit Broad Functionality and Define a Distinct Core Signaling Triad

Joe B. Blumer and Stephen M. Lanier
Molecular Pharmacology March 2014, 85 (3) 388-396; DOI: https://doi.org/10.1124/mol.113.090068
Joe B. Blumer
Department of Cell and Molecular Pharmacology and Experimental Therapeutics, Medical University of South Carolina, Charleston, South Carolina
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Stephen M. Lanier
Department of Cell and Molecular Pharmacology and Experimental Therapeutics, Medical University of South Carolina, Charleston, South Carolina
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Abstract

Activators of G protein signaling (AGS), initially discovered in the search for receptor-independent activators of G protein signaling, define a broad panel of biologic regulators that influence signal transfer from receptor to G-protein, guanine nucleotide binding and hydrolysis, G protein subunit interactions, and/or serve as alternative binding partners for Gα and Gβγ independently of the classic heterotrimeric Gαβγ. AGS proteins generally fall into three groups based upon their interaction with and regulation of G protein subunits: group I, guanine nucleotide exchange factors (GEF); group II, guanine nucleotide dissociation inhibitors; and group III, entities that bind to Gβγ. Group I AGS proteins can engage all subclasses of G proteins, whereas group II AGS proteins primarily engage the Gi/Go/transducin family of G proteins. A fourth group of AGS proteins with selectivity for Gα16 may be defined by the Mitf-Tfe family of transcription factors. Groups I–III may act in concert, generating a core signaling triad analogous to the core triad for heterotrimeric G proteins (GEF + G proteins + effector). These two core triads may function independently of each other or actually cross-integrate for additional signal processing. AGS proteins have broad functional roles, and their discovery has advanced new concepts in signal processing, cell and tissue biology, receptor pharmacology, and system adaptation, providing unexpected platforms for therapeutic and diagnostic development.

Footnotes

    • Received October 1, 2013.
    • Accepted December 3, 2013.
  • This work was supported by the National Institutes of Health National Institute of General Medical Sciences [Grants R01-GM086510 and R01-GM074247]; the National Institutes of Health National Institute of Neurological Disorders and Stroke [Grant R01-NS24821]; the National Institutes of Health National Institute on Drug Abuse [Grant R01-DA025896]; and the National Institutes of Health National Institute of Mental Health [Grant R01-MH59931].

  • dx.doi.org/10.1124/mol.113.090068.

  • Copyright © 2014 by The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 85 (3)
Molecular Pharmacology
Vol. 85, Issue 3
1 Mar 2014
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Rapid CommunicationMinireviews

Activators of G Protein Signaling (AGS Proteins)

Joe B. Blumer and Stephen M. Lanier
Molecular Pharmacology March 1, 2014, 85 (3) 388-396; DOI: https://doi.org/10.1124/mol.113.090068

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Rapid CommunicationMinireviews

Activators of G Protein Signaling (AGS Proteins)

Joe B. Blumer and Stephen M. Lanier
Molecular Pharmacology March 1, 2014, 85 (3) 388-396; DOI: https://doi.org/10.1124/mol.113.090068
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