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Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation

Author

Listed:
  • Guillaume Lebon

    (MRC Laboratory of Molecular Biology, Hills Road)

  • Tony Warne

    (MRC Laboratory of Molecular Biology, Hills Road)

  • Patricia C. Edwards

    (MRC Laboratory of Molecular Biology, Hills Road)

  • Kirstie Bennett

    (Heptares Therapeutics, BioPark, Broadwater Road)

  • Christopher J. Langmead

    (Heptares Therapeutics, BioPark, Broadwater Road)

  • Andrew G. W. Leslie

    (MRC Laboratory of Molecular Biology, Hills Road)

  • Christopher G. Tate

    (MRC Laboratory of Molecular Biology, Hills Road)

Abstract

Adenosine A2A receptor structure Adenosine receptors are G protein-coupled receptors that are found in the heart and the brain, and adenosine is the endogenous ligand for this class of transmembrane receptor. Lebon et al. present two X-ray crystal structures of a thermostabilized human adenosine A2A receptor bound to its endogenous agonist adenosine and the synthetic agonist NECA. Comparison of the agonist-bound structures of A2A receptor with the agonist-bound structures of β-adrenoceptors suggests that the contraction of the ligand binding pocket caused by the inward motion of several helices may be a common feature in the activation of all G protein-coupled receptors.

Suggested Citation

  • Guillaume Lebon & Tony Warne & Patricia C. Edwards & Kirstie Bennett & Christopher J. Langmead & Andrew G. W. Leslie & Christopher G. Tate, 2011. "Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation," Nature, Nature, vol. 474(7352), pages 521-525, June.
  • Handle: RePEc:nat:nature:v:474:y:2011:i:7352:d:10.1038_nature10136
    DOI: 10.1038/nature10136
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    Cited by:

    1. Hongmin Cai & Shimeng Guo & Youwei Xu & Jun Sun & Junrui Li & Zhikan Xia & Yi Jiang & Xin Xie & H. Eric Xu, 2024. "Cryo-EM structures of adenosine receptor A3AR bound to selective agonists," Nature Communications, Nature, vol. 15(1), pages 1-10, December.
    2. Yuxia Qian & Jiening Wang & Linlin Yang & Yanru Liu & Lina Wang & Wei Liu & Yun Lin & Hong Yang & Lixin Ma & Sheng Ye & Shan Wu & Anna Qiao, 2022. "Activation and signaling mechanism revealed by GPR119-Gs complex structures," Nature Communications, Nature, vol. 13(1), pages 1-10, December.
    3. Xudong Wang & Chris Neale & Soo-Kyung Kim & William A. Goddard & Libin Ye, 2023. "Intermediate-state-trapped mutants pinpoint G protein-coupled receptor conformational allostery," Nature Communications, Nature, vol. 14(1), pages 1-10, December.

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