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Structure and Activation Mechanism of GPCRs

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Structure and Function of GPCRs

Part of the book series: Topics in Medicinal Chemistry ((TMC,volume 30))

Abstract

G-protein-coupled receptors (GPCRs) mediate a wide variety of physiological functions and are a rich source of drug targets. In response to activation by extracellular stimuli, GPCRs trigger cytoplasmic signalling pathways through intracellular partners such as G-proteins and arrestins. This chapter provides a general overview of the molecular mechanisms of GPCR activation gleaned from crystal structures, biophysical experiments, and computational analyses. Furthermore, existing challenges and unresolved mechanistic questions about GPCR signalling are highlighted.

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Acknowledgments

The author acknowledges Stanford ChEM-H seed grant, Dror Lab, and Kobilka Lab at Stanford for supporting his research and Guillaume Lebon, Naomi R. Latorraca, Siri van Keulen, and Jonas Kaindl for critically reading the manuscript. The author has no conflicts of interests.

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Authors and Affiliations

  1. Department of Computer Science, Stanford University, Stanford, CA, USA

    A. J. Venkatakrishnan

  2. Department of Molecular and Cellular Physiology, Stanford University School of Medicine, Stanford, CA, USA

    A. J. Venkatakrishnan

  3. Institute for Computational and Mathematical Engineering, Stanford University, Stanford, CA, USA

    A. J. Venkatakrishnan

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  1. A. J. Venkatakrishnan
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Correspondence to A. J. Venkatakrishnan .

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Editors and Affiliations

  1. Institut de Génomique Fonctionnelle Centre National de la Recherche Scientifique (CNRS), Institut National de la Santé et de la Recherche Médicale (INSERM), University of Montpellier, Montpellier, France

    Guillaume Lebon

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Venkatakrishnan, A.J. (2019). Structure and Activation Mechanism of GPCRs. In: Lebon, G. (eds) Structure and Function of GPCRs. Topics in Medicinal Chemistry, vol 30. Springer, Cham. https://doi.org/10.1007/7355_2018_62

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