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Molecular Pharmacology

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Review ArticleMINIREVIEWS

Structure and Function of Heterotrimeric G Protein-Regulated Rho Guanine Nucleotide Exchange Factors

Mohamed Aittaleb, Cassandra A. Boguth and John J. G. Tesmer
Molecular Pharmacology February 2010, 77 (2) 111-125; DOI: https://doi.org/10.1124/mol.109.061234
Mohamed Aittaleb
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Cassandra A. Boguth
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John J. G. Tesmer
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Abstract

Activation of certain classes of G protein-coupled receptors (GPCRs) can lead to alterations in the actin cytoskeleton, gene transcription, cell transformation, and other processes that are known to be regulated by Rho family small-molecular-weight GTPases. Although these responses can occur indirectly via cross-talk from canonical heterotrimeric G protein cascades, it has recently been demonstrated that Dbl family Rho guanine nucleotide exchange factors (RhoGEFs) can serve as the direct downstream effectors of heterotrimeric G proteins. Heterotrimeric Gα12/13, Gαq, and Gβγ subunits are each now known to directly bind and regulate RhoGEFs. Atomic structures have recently been determined for several of these RhoGEFs and their G protein complexes, providing fresh insight into the molecular mechanisms of signal transduction between GPCRs and small molecular weight G proteins. This review covers what is currently known about the structure, function, and regulation of these recently recognized effectors of heterotrimeric G proteins.

Footnotes

  • This work was supported by National Institutes of Health National Heart, Lung, and Blood Institute [Grants HL086865, HL071818].

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

    doi:10.1124/mol.109.061234

  • ABBREVIATIONS:

    Dbs
    Dbl's big sister
    DEP
    Disheveled/EGL10/Pleckstrin
    DH
    Dbl homology
    GAP
    GTPase-activating protein
    GEF
    guanine nucleotide exchange factor
    GPCR
    G protein-coupled receptor
    HEK
    human embryonic kidney
    IP4P
    inositol polyphosphate-4-phosphatase
    LARG
    leukemia-associated RhoGEF
    Lbc
    lymphoid blast crisis
    LPA
    lysophosphatidic acid
    PDZ
    postsynaptic density 95, disk large, zona occludens-1
    PH
    pleckstrin homology
    PI3K
    phosphatidyl inositol-3 kinase
    PIP3
    phosphatidylinositol (3,4,5)-triphosphate
    PKA
    cAMP-dependent protein kinase
    PLC
    phospholipase C
    P-Rex
    PIP3-dependent Rac exchanger
    rgRGS
    RhoGEF fragment containing both N-terminal GAP motif and RH domain
    RGS
    regulators of G protein signaling
    RhoGEF
    Rho guanine nucleotide exchange factor
    RH
    RGS homology
    SH3
    Src homology 3
    SRF
    serum response factor.

  • Received September 22, 2009.
  • Accepted October 30, 2009.
  • Copyright © 2010 The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 77 (2)
Molecular Pharmacology
Vol. 77, Issue 2
1 Feb 2010
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Review ArticleMINIREVIEWS

Structure and Function of Heterotrimeric G Protein-Regulated Rho Guanine Nucleotide Exchange Factors

Mohamed Aittaleb, Cassandra A. Boguth and John J. G. Tesmer
Molecular Pharmacology February 1, 2010, 77 (2) 111-125; DOI: https://doi.org/10.1124/mol.109.061234

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Review ArticleMINIREVIEWS

Structure and Function of Heterotrimeric G Protein-Regulated Rho Guanine Nucleotide Exchange Factors

Mohamed Aittaleb, Cassandra A. Boguth and John J. G. Tesmer
Molecular Pharmacology February 1, 2010, 77 (2) 111-125; DOI: https://doi.org/10.1124/mol.109.061234
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