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Conformational Plasticity of GPCR Binding Sites

Structural Basis for Evolutionary Diversity in Ligand Recognition

  • Chapter
The G Protein-Coupled Receptors Handbook

Part of the book series: Contemporary Clinical Neuroscience ((CCNE))

Abstract

Genome sequencing projects have identified the G protein-coupled receptor (GPCR) superfamily as one of the largest classes of proteins in mammalian genomes (1). For example, preliminary analyses of the human genome have revealed up to 600 GPCRs (2,3). Additionally, GPCRs are scored as the most common family in the human proteome at the Proteome Analysis Database of the European Bioinformatics Institute(see http://www.ebi.ac.uk/proteome/HUMAN/interpro/top15f.html), with more than 800 sequences. Based on phylogenetic analyses of the human genome, these receptors have been classified into five main families: glutamate, rhodopsin, adhesion, frizzled/taste2, and secretin (4).

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Author information

Authors and Affiliations

  1. Department of Molecular & Cellular Physiology, Stanford University, Palo Alto, California

    Xavier Deupi PhD

  2. Department of Cellular, University of California, San Francisco, California

    Cedric Govaerts PhD

  3. Department of Molecular Pharmacology, University of California, San Francisco, California

    Cedric Govaerts PhD

  4. Institute for Computational Biomedicine, Weill Medical College of Cornell University, New York, NY

    Lei Shi PhD

  5. Center for Molecular Recognition, Columbia University College of Physicians & Surgeons, New York, NY

    Jonathan A. Javitch MD, PhD

  6. Laboratori de Medicina Computacional, Unitat de Bioestadística and Institut de Neurociències, Universitat Autònoma de Barcelona, Bellaterra, Catalunya, Spain

    Leonardo Pardo PhD

  7. Novasite Pharmaceuticals Inc., San Diego, CA

    Juan Ballesteros PhD (Chief Scientific Officer)

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  1. Xavier Deupi PhD
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  2. Cedric Govaerts PhD
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  3. Lei Shi PhD
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  4. Jonathan A. Javitch MD, PhD
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  5. Leonardo Pardo PhD
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  6. Juan Ballesteros PhD
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Editor information

Editors and Affiliations

  1. Department of Pharmacology and Biological Chemistry, Mount Sinai School of Medicine, New York, NY

    Lakshmi A. Devi PhD

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© 2005 Humana Press Inc., Totowa, NJ

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Deupi, X., Govaerts, C., Shi, L., Javitch, J.A., Pardo, L., Ballesteros, J. (2005). Conformational Plasticity of GPCR Binding Sites. In: Devi, L.A. (eds) The G Protein-Coupled Receptors Handbook. Contemporary Clinical Neuroscience. Humana Press. https://doi.org/10.1007/978-1-59259-919-6_17

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