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Structure of CC chemokine receptor 2 with orthosteric and allosteric antagonists

Author

Listed:
  • Yi Zheng

    (Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, 9500 Gilman Drive,)

  • Ling Qin

    (Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, 9500 Gilman Drive,)

  • Natalia V. Ortiz Zacarías

    (Leiden Academic Centre for Drug Research (LACDR), Leiden University, Leiden 2333 CC, The Netherlands)

  • Henk de Vries

    (Leiden Academic Centre for Drug Research (LACDR), Leiden University, Leiden 2333 CC, The Netherlands)

  • Gye Won Han

    (Bridge Institute, University of Southern California)

  • Martin Gustavsson

    (Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, 9500 Gilman Drive,)

  • Marta Dabros

    (Bristol-Myers Squibb Company)

  • Chunxia Zhao

    (Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, 9500 Gilman Drive,)

  • Robert J. Cherney

    (Bristol-Myers Squibb Company)

  • Percy Carter

    (Bristol-Myers Squibb Company)

  • Dean Stamos

    (Vertex Pharmaceuticals Inc.)

  • Ruben Abagyan

    (Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, 9500 Gilman Drive,)

  • Vadim Cherezov

    (Bridge Institute, University of Southern California)

  • Raymond C. Stevens

    (The Bridge Institute, University of Southern California)

  • Adriaan P. IJzerman

    (Leiden Academic Centre for Drug Research (LACDR), Leiden University, Leiden 2333 CC, The Netherlands)

  • Laura H. Heitman

    (Leiden Academic Centre for Drug Research (LACDR), Leiden University, Leiden 2333 CC, The Netherlands)

  • Andrew Tebben

    (Bristol-Myers Squibb Company)

  • Irina Kufareva

    (Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, 9500 Gilman Drive,)

  • Tracy M. Handel

    (Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, 9500 Gilman Drive,)

Abstract

The crystal structure of CCR2 chemokine receptor in a complex with two different antagonists—one orthosteric the other allosteric—which functionally cooperate to inhibit CCR2.

Suggested Citation

  • Yi Zheng & Ling Qin & Natalia V. Ortiz Zacarías & Henk de Vries & Gye Won Han & Martin Gustavsson & Marta Dabros & Chunxia Zhao & Robert J. Cherney & Percy Carter & Dean Stamos & Ruben Abagyan & Vadim, 2016. "Structure of CC chemokine receptor 2 with orthosteric and allosteric antagonists," Nature, Nature, vol. 540(7633), pages 458-461, December.
    • Handle: RePEc:nat:nature:v:540:y:2016:i:7633:d:10.1038_nature20605
    DOI: 10.1038/nature20605
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    Cited by:

    1. David Jonathan Wasilko & Brian S. Gerstenberger & Kathleen A. Farley & Wei Li & Jennifer Alley & Mark E. Schnute & Ray J. Unwalla & Jorge Victorino & Kimberly K. Crouse & Ru Ding & Parag V. Sahasrabud, 2024. "Structural basis for CCR6 modulation by allosteric antagonists," Nature Communications, Nature, vol. 15(1), pages 1-13, December.
    2. Janik B. Hedderich & Margherita Persechino & Katharina Becker & Franziska M. Heydenreich & Torben Gutermuth & Michel Bouvier & Moritz Bünemann & Peter Kolb, 2022. "The pocketome of G-protein-coupled receptors reveals previously untargeted allosteric sites," Nature Communications, Nature, vol. 13(1), pages 1-12, December.
    3. Dawei Sun & Yonglian Sun & Eric Janezic & Tricia Zhou & Matthew Johnson & Caleigh Azumaya & Sigrid Noreng & Cecilia Chiu & Akiko Seki & Teresita L. Arenzana & John M. Nicoludis & Yongchang Shi & Baome, 2023. "Structural basis of antibody inhibition and chemokine activation of the human CC chemokine receptor 8," Nature Communications, Nature, vol. 14(1), pages 1-13, December.

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