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High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875

Author

Listed:
  • Ankita Srivastava

    (Takeda California, 10410 Science Center Drive)

  • Jason Yano

    (Takeda California, 10410 Science Center Drive)

  • Yoshihiko Hirozane

    (Biomolecular Research Laboratories, Takeda Pharmaceutical Company Ltd, 26-1, Muraoka-Higashi 2-chome, Fujisawa, Kanagawa 251-8555, Japan)

  • Georgia Kefala

    (Takeda California, 10410 Science Center Drive)

  • Franz Gruswitz

    (Takeda California, 10410 Science Center Drive
    Present addresses: Beryllium, Membrane Protein Sciences, 7869 NE Day Road West, Bainbridge Island, Washington 98110, USA (F.G.); Dart Neuroscience, 12278 Scripps Summit Drive, San Diego, California 92131, USA (K.A. and J.N.).)

  • Gyorgy Snell

    (Takeda California, 10410 Science Center Drive)

  • Weston Lane

    (Takeda California, 10410 Science Center Drive)

  • Anthony Ivetac

    (Takeda California, 10410 Science Center Drive)

  • Kathleen Aertgeerts

    (Takeda California, 10410 Science Center Drive
    Present addresses: Beryllium, Membrane Protein Sciences, 7869 NE Day Road West, Bainbridge Island, Washington 98110, USA (F.G.); Dart Neuroscience, 12278 Scripps Summit Drive, San Diego, California 92131, USA (K.A. and J.N.).)

  • Jasmine Nguyen

    (Takeda California, 10410 Science Center Drive
    Present addresses: Beryllium, Membrane Protein Sciences, 7869 NE Day Road West, Bainbridge Island, Washington 98110, USA (F.G.); Dart Neuroscience, 12278 Scripps Summit Drive, San Diego, California 92131, USA (K.A. and J.N.).)

  • Andy Jennings

    (Takeda California, 10410 Science Center Drive)

  • Kengo Okada

    (Biomolecular Research Laboratories, Takeda Pharmaceutical Company Ltd, 26-1, Muraoka-Higashi 2-chome, Fujisawa, Kanagawa 251-8555, Japan)

Abstract

The X-ray crystal structure of human GPR40 receptor in the presence of TAK-875, an orally available, potent and selective human GPR40 agonist.

Suggested Citation

  • Ankita Srivastava & Jason Yano & Yoshihiko Hirozane & Georgia Kefala & Franz Gruswitz & Gyorgy Snell & Weston Lane & Anthony Ivetac & Kathleen Aertgeerts & Jasmine Nguyen & Andy Jennings & Kengo Okada, 2014. "High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875," Nature, Nature, vol. 513(7516), pages 124-127, September.
  • Handle: RePEc:nat:nature:v:513:y:2014:i:7516:d:10.1038_nature13494
    DOI: 10.1038/nature13494
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    Cited by:

    1. Xin Chen & Kexin Wang & Jianfang Chen & Chao Wu & Jun Mao & Yuanpeng Song & Yijing Liu & Zhenhua Shao & Xuemei Pu, 2024. "Integrative residue-intuitive machine learning and MD Approach to Unveil Allosteric Site and Mechanism for β2AR," Nature Communications, Nature, vol. 15(1), pages 1-17, December.
    2. Joshua A. Lees & João M. Dias & Francis Rajamohan & Jean-Philippe Fortin & Rebecca O’Connor & Jimmy X. Kong & Emily A. G. Hughes & Ethan L. Fisher & Jamison B. Tuttle & Gabrielle Lovett & Bethany L. K, 2023. "An inverse agonist of orphan receptor GPR61 acts by a G protein-competitive allosteric mechanism," Nature Communications, Nature, vol. 14(1), pages 1-12, December.

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