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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מידע ביבליוגרפי

Principais autores:	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
פורמט:	Artigo
שפה:	Inglês
יצא לאור:	Nature Portfolio 2020-12-01
סדרה:	Communications Biology
גישה מקוונת:	https://doi.org/10.1038/s42003-020-01504-0
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