Structural insight into allosteric modulation of protease-activated receptor 2

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, Christoph Grebner, Nils-Olov Hermansson, Ali Jazayeri, Patrik Johansson, Louis Leong, Rudi Prihandoko, Mathieu Rappas, Holly Soutter, Arjan Snijder, Linda Sundström, Benjamin Tehan, Peter Thornton, Dawn Troast, Giselle Wiggin, Andrei Zhukov, Fiona H. Marshall () and Niek Dekker
Additional contact information
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

Nature, 2017, vol. 545, issue 7652, 112-115

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.

Date: 2017
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DOI: 10.1038/nature22309

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