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      Strike a pose: Gαq complexes at the membrane.

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          Abstract

          The heterotrimeric G protein Gαq is a central player in signal transduction, relaying signals from activated G-protein-coupled receptors (GPCRs) to effectors and other proteins to elicit changes in intracellular Ca(2+), the actin cytoskeleton, and gene transcription. Gαq functions at the intracellular surface of the plasma membrane, as do its best-characterized targets, phospholipase C-β, p63RhoGEF, and GPCR kinase 2 (GRK2). Recent insights into the structure and function of these signaling complexes reveal several recurring themes, including complex multivalent interactions between Gαq, its protein target, and the membrane, that are likely essential for allosteric control and maximum efficiency in signal transduction. Thus, the plasma membrane is not only a source of substrates but also a key player in the scaffolding of Gαq-dependent signaling pathways.

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          Author and article information

          Journal
          Trends Pharmacol. Sci.
          Trends in pharmacological sciences
          Elsevier BV
          1873-3735
          0165-6147
          Jan 2014
          : 35
          : 1
          Affiliations
          [1 ] Life Sciences Institute and the Departments of Pharmacology and Biological Chemistry, University of Michigan, Ann Arbor, MI, USA.
          [2 ] Life Sciences Institute and the Departments of Pharmacology and Biological Chemistry, University of Michigan, Ann Arbor, MI, USA. Electronic address: tesmerjj@umich.edu.
          Article
          S0165-6147(13)00204-6 NIHMS535432
          10.1016/j.tips.2013.10.008
          3880608
          24287282
          b849729c-cae6-4680-87bb-2a9126393c6b
          History

          ARHGEF25,G-protein-coupled receptor,GRK2,Gα(q),crystallography,heterotrimeric G protein signaling,membrane,p63RhoGEF,phospholipase Cβ,phospholipids,protein structure,second messengers

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