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Transmembrane Signaling Protocols pp 3–49Cite as

Transmembrane Signaling by G Protein-Coupled Receptors

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Part of the book series: Methods in Molecular Biology™ ((MIMB,volume 332))

Summary

G protein-coupled receptors (GPCRs) make up the largest and most diverse family of membrane receptors in the human genome, relaying information about the presence of diverse extracellular stimuli to the cell interior. All known GPCRs share a common architecture of seven membrane-spanning helices connected by intra- and extracellular loops. Most GPCR-mediated cellular responses result from the receptor acting as a ligand-activated guanine nucleotide exchange factor for heterotrimeric guanine nucleotide-binding (G) proteins whose dissociated subunits activate effector enzymes or ion chan-nels. GPCR signaling is subject to extensive negative regulation through receptor desensitization, sequestration, and down regulation, termination of G protein activation by GTPase-activation proteins, and enzymatic degradation of second messengers. Addi-tional protein—protein interactions positively modulate GPCR signaling by influencing ligand-binding affinity and specificity, coupling between receptors, G proteins and effectors, or targeting to specific subcellular locations. These include the formation of GPCR homo- and heterodimers, the interaction of GPCRs with receptor activity-modi-fying proteins, and the binding of various scaffolding proteins to intracellular receptor domains. In some cases, these processes appear to generate signals in conjunction with, or even independent of, G protein activation.

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Authors and Affiliations

  1. Department of Medicine and Biochemistry and Molecular Biology, Medical University of South Carolina, Charleston, SC

    Louis M. Luttrell

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Editors and Affiliations

  1. Department of Pathology, School of Dental Medicine, The University of Pennsylvania, Philadelphia, PA

    Hydar Ali

  2. Department of Microbiology and Immunology, James Graham Brown Cancer Center, University of Louisville, Louisville, KY

    Bodduluri Haribabu

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Luttrell, L.M. (2006). Transmembrane Signaling by G Protein-Coupled Receptors. In: Ali, H., Haribabu, B. (eds) Transmembrane Signaling Protocols. Methods in Molecular Biology™, vol 332. Humana Press. https://doi.org/10.1385/1-59745-048-0:1

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  • DOI: https://doi.org/10.1385/1-59745-048-0:1

  • Publisher Name: Humana Press

  • Print ISBN: 978-1-58829-546-0

  • Online ISBN: 978-1-59745-048-5

  • eBook Packages: Springer Protocols

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