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Conformational dynamics of a class C G-protein-coupled receptor

Author

Listed:
  • Reza Vafabakhsh

    (University of California)

  • Joshua Levitz

    (University of California)

  • Ehud Y. Isacoff

    (University of California
    Helen Wills Neuroscience Institute, University of California
    Lawrence Berkeley National Laboratory)

Abstract

smFRET is used to probe the activation mechanism of two full-length mammalian glutamate receptors, revealing that the extracellular ligand-binding domains of these G-protein-coupled receptors interconvert between three confirmations (resting, activated and a short-lived intermediate state), and that the efficacy of an orthosteric agonist correlates with the degree of occupancy of the active state.

Suggested Citation

  • Reza Vafabakhsh & Joshua Levitz & Ehud Y. Isacoff, 2015. "Conformational dynamics of a class C G-protein-coupled receptor," Nature, Nature, vol. 524(7566), pages 497-501, August.
    • Handle: RePEc:nat:nature:v:524:y:2015:i:7566:d:10.1038_nature14679
    DOI: 10.1038/nature14679
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    Citations

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    Cited by:

    1. Chris Habrian & Naomi Latorraca & Zhu Fu & Ehud Y. Isacoff, 2023. "Homo- and hetero-dimeric subunit interactions set affinity and efficacy in metabotropic glutamate receptors," Nature Communications, Nature, vol. 14(1), pages 1-10, December.
    2. Mingyu Li & Xiaobing Lan & Xinchao Shi & Chunhao Zhu & Xun Lu & Jun Pu & Shaoyong Lu & Jian Zhang, 2024. "Delineating the stepwise millisecond allosteric activation mechanism of the class C GPCR dimer mGlu5," Nature Communications, Nature, vol. 15(1), pages 1-14, December.
    3. Alexa Strauss & Alberto J. Gonzalez-Hernandez & Joon Lee & Nohely Abreu & Purushotham Selvakumar & Leslie Salas-Estrada & Melanie Kristt & Anisul Arefin & Kevin Huynh & Dagan C. Marx & Kristen Gillila, 2024. "Structural basis of positive allosteric modulation of metabotropic glutamate receptor activation and internalization," Nature Communications, Nature, vol. 15(1), pages 1-17, December.
    4. Michael R. Schamber & Reza Vafabakhsh, 2022. "Mechanism of sensitivity modulation in the calcium-sensing receptor via electrostatic tuning," Nature Communications, Nature, vol. 13(1), pages 1-14, December.

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