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Structural insight into allosteric modulation of protease-activated receptor 2

Author

Listed:
  • Robert K. Y. Cheng

    (Heptares Therapeutics Ltd, BioPark, Broadwater Road, Welwyn Garden City)

  • Cédric Fiez-Vandal

    (Heptares Therapeutics Ltd, BioPark, Broadwater Road, Welwyn Garden City)

  • Oliver Schlenker

    (Heptares Therapeutics Ltd, BioPark, Broadwater Road, Welwyn Garden City)

  • Karl Edman

    (Discovery Sciences, Innovative Medicines and Early Development Biotech Unit)

  • Birte Aggeler

    (Bio-techne, 614 McKinley Place NE)

  • Dean G. Brown

    (Discovery Sciences, Innovative Medicines and Early Development Biotech Unit, AstraZeneca R&D)

  • Giles A. Brown

    (Heptares Therapeutics Ltd, BioPark, Broadwater Road, Welwyn Garden City)

  • Robert M. Cooke

    (Heptares Therapeutics Ltd, BioPark, Broadwater Road, Welwyn Garden City)

  • Christoph E. Dumelin

    (X-Chem Inc., 100 Beaver St.)

  • Andrew S. Doré

    (Heptares Therapeutics Ltd, BioPark, Broadwater Road, Welwyn Garden City)

  • Stefan Geschwindner

    (Discovery Sciences, Innovative Medicines and Early Development Biotech Unit)

  • Christoph Grebner

    (Cardiovascular and Metabolic Diseases, Innovative Medicines and Early Development Biotech Unit, AstraZeneca)

  • Nils-Olov Hermansson

    (Discovery Sciences, Innovative Medicines and Early Development Biotech Unit)

  • Ali Jazayeri

    (Heptares Therapeutics Ltd, BioPark, Broadwater Road, Welwyn Garden City)

  • Patrik Johansson

    (Discovery Sciences, Innovative Medicines and Early Development Biotech Unit)

  • Louis Leong

    (Bio-techne, 614 McKinley Place NE)

  • Rudi Prihandoko

    (Heptares Therapeutics Ltd, BioPark, Broadwater Road, Welwyn Garden City)

  • Mathieu Rappas

    (Heptares Therapeutics Ltd, BioPark, Broadwater Road, Welwyn Garden City)

  • Holly Soutter

    (X-Chem Inc., 100 Beaver St.)

  • Arjan Snijder

    (Discovery Sciences, Innovative Medicines and Early Development Biotech Unit)

  • Linda Sundström

    (Discovery Sciences, Innovative Medicines and Early Development Biotech Unit)

  • Benjamin Tehan

    (Heptares Therapeutics Ltd, BioPark, Broadwater Road, Welwyn Garden City)

  • Peter Thornton

    (Neuroscience, Innovative Medicines and Early Development Biotech Unit, AstraZeneca)

  • Dawn Troast

    (X-Chem Inc., 100 Beaver St.)

  • Giselle Wiggin

    (Heptares Therapeutics Ltd, BioPark, Broadwater Road, Welwyn Garden City)

  • Andrei Zhukov

    (Heptares Therapeutics Ltd, BioPark, Broadwater Road, Welwyn Garden City)

  • Fiona H. Marshall

    (Heptares Therapeutics Ltd, BioPark, Broadwater Road, Welwyn Garden City)

  • Niek Dekker

    (Discovery Sciences, Innovative Medicines and Early Development Biotech Unit)

Abstract

Crystal structures of protease-activated receptor 2 (PAR2) in complex with two different antagonist ligands and with a blocking antibody reveal binding sites that are distinct from those found on PAR1, offering new leads for structure-based drug design.

Suggested Citation

  • Robert K. Y. Cheng & Cédric Fiez-Vandal & Oliver Schlenker & Karl Edman & Birte Aggeler & Dean G. Brown & Giles A. Brown & Robert M. Cooke & Christoph E. Dumelin & Andrew S. Doré & Stefan Geschwindner, 2017. "Structural insight into allosteric modulation of protease-activated receptor 2," Nature, Nature, vol. 545(7652), pages 112-115, May.
    • Handle: RePEc:nat:nature:v:545:y:2017:i:7652:d:10.1038_nature22309
    DOI: 10.1038/nature22309
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