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Molecular Pharmacology

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Research ArticleMINIREVIEWS

Thinking Outside of the “RGS Box”: New Approaches to Therapeutic Targeting of Regulators of G Protein Signaling

Benita Sjögren and Richard R. Neubig
Molecular Pharmacology October 2010, 78 (4) 550-557; DOI: https://doi.org/10.1124/mol.110.065219
Benita Sjögren
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Richard R. Neubig
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Abstract

Regulators of G protein signaling (RGS) proteins are emerging as potentially important drug targets. The mammalian RGS protein family has more than 20 members and they share a common ∼120-residue RGS homology domain or “RGS box.” RGS proteins regulate signaling via G protein-coupled receptors by accelerating GTPase activity at active α subunits of G proteins of the Gq and Gi/o families. Most studies searching for modulators of RGS protein function have been focused on inhibiting the GTPase accelerating protein activity. However, many RGS proteins contain additional domains that serve other functions, such as interactions with proteins or subcellular targeting. Here, we discuss a rationale for therapeutic targeting of RGS proteins by regulation of expression or allosteric modulation to permit either increases or decreases in RGS function. Several RGS proteins have reduced expression or function in pathophysiological states, so strategies to increase RGS function would be useful. Because several RGS proteins are rapidly degraded by the N-end rule pathway, finding ways to stabilize them may prove to be an effective way to enhance RGS protein function.

Footnotes

  • This work was supported by the National Institutes of Health National Institute of General Medical Sciences [Grant R01-GM39561] and The Swedish Research council [Grant VR-524-2008-6963].

  • Article, publication date, and citation information can be found at http://molpharm.aspetjournals.org.

    doi:10.1124/mol.110.065219.

  • ABBREVIATIONS:

    GPCR
    G protein-coupled receptor
    RGS
    regulators of G protein signaling
    GAP
    GTPase-accelerating protein
    RH
    RGS homology
    AC
    adenylate cyclase
    DEP
    disheveled-EGL10-Pleckstrin homology
    R7BP
    R7 binding protein
    GGL
    Gγ-like
    CCG-4986
    [methyl-N-[(4-chlorophenyl)sulfonyl]-4-nitrobenzenesulfinimidoate]
    NPI-0052
    Salinosporamide A
    HEK
    human embryonic kidney
    MG-132
    N-benzoyloxycarbonyl (Z)-Leu-Leu-leucinal.

  • Received March 31, 2010.
  • Accepted July 22, 2010.
  • Copyright © 2010 The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 78 (4)
Molecular Pharmacology
Vol. 78, Issue 4
1 Oct 2010
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Research ArticleMINIREVIEWS

Thinking Outside of the “RGS Box”: New Approaches to Therapeutic Targeting of Regulators of G Protein Signaling

Benita Sjögren and Richard R. Neubig
Molecular Pharmacology October 1, 2010, 78 (4) 550-557; DOI: https://doi.org/10.1124/mol.110.065219

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Research ArticleMINIREVIEWS

Thinking Outside of the “RGS Box”: New Approaches to Therapeutic Targeting of Regulators of G Protein Signaling

Benita Sjögren and Richard R. Neubig
Molecular Pharmacology October 1, 2010, 78 (4) 550-557; DOI: https://doi.org/10.1124/mol.110.065219
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