Structural insight into allosteric modulation of protease-activated receptor 2

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. PAR2 structures shed light on allosteric mecha...

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Veröffentlicht in:	Nature (London) Jg. 545; H. 7652; S. 112 - 115
Hauptverfasser:	Cheng, Robert K. Y., Fiez-Vandal, Cédric, Schlenker, Oliver, Edman, Karl, Aggeler, Birte, Brown, Dean G., Brown, Giles A., Cooke, Robert M., Dumelin, Christoph E., Doré, Andrew S., Geschwindner, Stefan, Grebner, Christoph, Hermansson, Nils-Olov, Jazayeri, Ali, Johansson, Patrik, Leong, Louis, Prihandoko, Rudi, Rappas, Mathieu, Soutter, Holly, Snijder, Arjan, Sundström, Linda, Tehan, Benjamin, Thornton, Peter, Troast, Dawn, Wiggin, Giselle, Zhukov, Andrei, Marshall, Fiona H., Dekker, Niek
Format:	Journal Article
Sprache:	Englisch
Veröffentlicht:	London Nature Publishing Group UK 04.05.2017 Nature Publishing Group
Schlagworte:	101/1 631/154/436/2387 631/535/1266 631/92/436 98 Allosteric properties Allosteric proteins Allosteric Regulation - drug effects Allosteric Site - drug effects Antagonist drugs Antagonists Antibodies Antibodies, Blocking - chemistry Antibodies, Blocking - pharmacology Antigens Benzimidazoles - chemistry Benzimidazoles - pharmacology Benzodioxoles - chemistry Benzodioxoles - pharmacology Benzyl Alcohols - chemistry Benzyl Alcohols - pharmacology Binding sites Blocking antibodies Cell receptors Crystal structure Crystallography, X-Ray G protein-coupled receptors Homology Humanities and Social Sciences Humans Imidazoles - chemistry Imidazoles - pharmacology Immunoglobulin Fab Fragments - chemistry Immunoglobulin Fab Fragments - pharmacology Inflammation Isoforms Kinetics letter Ligands Models, Molecular Molecular structure multidisciplinary Mutation Peptides Physiological aspects Protease Proteins Proteolysis Receptor mechanisms Receptor, PAR-2 - antagonists & inhibitors Receptor, PAR-2 - chemistry Receptor, PAR-2 - metabolism Receptors Science Signal Transduction - drug effects Thromboembolism Thrombosis
ISSN:	0028-0836, 1476-4687, 1476-4687
Online-Zugang:	Volltext
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