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Estimation of the receptor-state affinity constants of ligands in functional studies using wild type and constitutively active mutant receptors: Implications for estimation of agonist bias

We describe a method for estimating the affinities of ligands for active and inactive states of a G protein-coupled receptor (GPCR). Our protocol involves measuring agonist-induced signaling responses of a wild type GPCR and a constitutively active mutant of it under control conditions and after par...

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Detalhes bibliográficos
Publicado no:J Pharmacol Toxicol Methods
Main Authors: Ehlert, Frederick J., Stein, Richard S.L.
Formato: Artigo
Idioma:Inglês
Publicado em: 2016
Assuntos:
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC5769967/
https://ncbi.nlm.nih.gov/pubmed/27725245
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.vascn.2016.09.007
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