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Purification and Crystallization of a Thermostabilized Agonist-Bound Conformation of the Human Adenosine A2A Receptor

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G Protein-Coupled Receptors in Drug Discovery

Part of the book series: Methods in Molecular Biology ((MIMB,volume 1335))

Abstract

Crystallization of G protein-coupled receptors (GPCRs) is successful due to the development of generic protein engineering strategies, which has resulted in the structure determination of more than 25 GPCRs, including representatives from class A, B, C, and F. Most of the X-ray structures available correspond to an inactive conformation of the receptor bound to an antagonist. Only a few high-resolution structures of agonist-bound conformations of GPCRs have been determined over the last 6 years. Here, we describe the purification and crystallization protocols of a thermostabilized agonist-bound conformation of the human adenosine A2A receptor.

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Authors and Affiliations

  1. MRC Laboratory of Molecular Biology, Cambridge Biomedical Campus, Francis Crick Avenue, Cambridge, CB2 0QH, UK

    Christopher G. Tate

  2. Institut de Génomique Fonctionnelle, UMR CNRS 5203, INSERM U1191, Université de Montpellier, 141 rue de la cardonille, 34094, Montpellier, Cedex 05, France

    Guillaume Lebon

Authors
  1. Christopher G. Tate
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  2. Guillaume Lebon
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Corresponding authors

Correspondence to Christopher G. Tate or Guillaume Lebon .

Editor information

Editors and Affiliations

  1. Department of Structural and Chemical Biology, Icahn School of Medicine at Mount Sinai, New York, New York, USA

    Marta Filizola

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Tate, C.G., Lebon, G. (2015). Purification and Crystallization of a Thermostabilized Agonist-Bound Conformation of the Human Adenosine A2A Receptor. In: Filizola, M. (eds) G Protein-Coupled Receptors in Drug Discovery. Methods in Molecular Biology, vol 1335. Humana Press, New York, NY. https://doi.org/10.1007/978-1-4939-2914-6_2

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  • DOI: https://doi.org/10.1007/978-1-4939-2914-6_2

  • Publisher Name: Humana Press, New York, NY

  • Print ISBN: 978-1-4939-2913-9

  • Online ISBN: 978-1-4939-2914-6

  • eBook Packages: Springer Protocols

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