Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhibition

Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhibition

Kennedy et al. report the pharmacological and in vivo profiling of two small molecule PAR2 inhibitors and an agonist. They conclude that while the small molecule agonist and one of the inhibitors bind to the orthosteric PAR2 binding site, the other inhibitor is a negative allosteric modulator, highl...

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Bibliographic Details
Main Authors: Amanda J. Kennedy, Linda Sundström, Stefan Geschwindner, Eunice K. Y. Poon, Yuhong Jiang, Rongfeng Chen, Rob Cooke, Shawn Johnstone, Andrew Madin, Junxian Lim, Qingqi Liu, Rink-Jan Lohman, Anneli Nordqvist, Maria Fridén-Saxin, Wenzhen Yang, Dean G. Brown, David P. Fairlie, Niek Dekker
Format: Article
Language:English
Published: Nature Publishing Group 2020-12-01
Series:Communications Biology
Online Access:https://doi.org/10.1038/s42003-020-01504-0

Internet

https://doi.org/10.1038/s42003-020-01504-0

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