Allosteric modulators enhance agonist efficacy by increasing the residence time of a GPCR in the active state

Much hope in drug development comes from the discovery of positive allosteric modulators (PAM) that display target subtype selectivity and act by increasing agonist potency and efficacy. How such compounds can allosterically influence agonist action remains unclear. Metabotropic glutamate receptors...

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Detalles Bibliográficos
Autores principales: Cao, Anne-Marinette, Quast, Robert B., Fatemi, Fataneh, Rondard, Philippe, Pin, Jean-Philippe, Margeat, Emmanuel
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2021
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8440590/
https://www.ncbi.nlm.nih.gov/pubmed/34521824
http://dx.doi.org/10.1038/s41467-021-25620-5

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8440590/
https://www.ncbi.nlm.nih.gov/pubmed/34521824
http://dx.doi.org/10.1038/s41467-021-25620-5

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