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β2-Adrenergic Receptor Activation by Agonists Studied with 19F NMR Spectroscopy

Authors

  • Dr. Reto Horst,

    1. Department of Integrative Structural and Computational Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037 (USA)
    2. Present address: Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT 06340 (USA)
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  • Jeffrey J. Liu,

    1. Department of Integrative Structural and Computational Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037 (USA)
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  • Prof. Dr. Raymond C. Stevens,

    1. Department of Integrative Structural and Computational Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037 (USA)
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  • Prof. Dr. Kurt Wüthrich

    Corresponding author
    1. Department of Integrative Structural and Computational Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037 (USA)
    2. Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037 (USA)
    • Department of Integrative Structural and Computational Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037 (USA)
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  • This work was supported by the NIH Roadmap initiative grant P50 GM073197 for technology development and the PSI:Biology grant U54 GM094618 for the GPCR-Network. K.W. is the Cecil H. and Ida M. Green Prof. of Structural Biology at The Scripps Research Institute. We thank Katya Kadyshevskaya for help with the illustrations.

Abstract

original image

Proteine in Zeitlupe: 19F-NMR-Studien deuten darauf hin, dass Übergänge zwischen aktiven und inaktiven Zuständen des humanen β2-adrenergen Rezeptors erhebliche Strukturumwandlungen erfordern (siehe Bild). Dies zeigt sich an der Enthalpiedifferenz ΔHo≈40 kJ mol−1 und einer langsamen Umwandlungsgeschwindigkeit mit kex≪10 s−1.

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