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

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 t...

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Detalles Bibliográficos
Autores principales: 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., Dekker, Niek
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2020
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7747594/
https://www.ncbi.nlm.nih.gov/pubmed/33335291
http://dx.doi.org/10.1038/s42003-020-01504-0

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7747594/
https://www.ncbi.nlm.nih.gov/pubmed/33335291
http://dx.doi.org/10.1038/s42003-020-01504-0

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