Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhib...
Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhibition
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Author / Creator
Kennedy, Amanda J. , Sundström, Linda , Geschwindner, Stefan , Poon, Eunice K. Y. , Jiang, Yuhong , Chen, Rongfeng , Cooke, Rob , Johnstone, Shawn , Madin, Andrew , Lim, Junxian , Liu, Qingqi , Lohman, Rink-Jan , Nordqvist, Anneli , Fridén-Saxin, Maria , Yang, Wenzhen , Brown, Dean G. , Fairlie, David P. and Dekker, Niek
Publisher
London: Nature Publishing Group UK
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English
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London: Nature Publishing Group UK
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Contents
Protease-activated receptor-2 (PAR2) has been implicated in multiple pathophysiologies but drug discovery is challenging due to low small molecule tractability and a complex activation mechanism. Here we report the pharmacological profiling of a potent new agonist, suggested by molecular modelling to bind in the putative orthosteric site, and two n...
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Full title
Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhibition
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TN_cdi_doaj_primary_oai_doaj_org_article_e6a39fb1480d47f3b76e5e7e14d4b26c
Permalink
https://devfeature-collection.sl.nsw.gov.au/record/TN_cdi_doaj_primary_oai_doaj_org_article_e6a39fb1480d47f3b76e5e7e14d4b26c
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ISSN
2399-3642
E-ISSN
2399-3642
DOI
10.1038/s42003-020-01504-0
