A Complementary Scale of Biased Agonism for Agonists with Differing Maximal Responses.

ABSTRACT: Compelling data in the literature from the recent years leave no doubt about the pluridimensional nature of G protein-coupled receptor function and the fact that some ligands can couple with different efficacies to the multiple pathways that a receptor can signal through, a phenomenon most commonly known as functional selectivity or biased agonism. Nowadays, transduction coefficients (log(τ/K_A)), based on the Black and Leff operational model of agonism, are widely used to calculate bias. Nevertheless, combining both affinity and efficacy in a single parameter can result in compounds showing a defined calculated bias of one pathway over other though displaying varying experimental bias preferences. In this paper, we present a novel scale (log(τ)), that attempts to give extra subs

SUBMITTER: Burgueno J 

PROVIDER: S-EPMC5684405 | biostudies-literature | 2017 Nov

REPOSITORIES: biostudies-literature