Premium
Quantifying Signaling Bias: A Simple Approach to Quantify Functional Selectivity and Agonist Bias
Author(s) -
Charter Neil,
Anantharaman Lakshmi
Publication year - 2015
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.29.1_supplement.lb468
Subject(s) - functional selectivity , internalization , g protein coupled receptor , agonist , signal transduction , receptor , ligand (biochemistry) , chemistry , biology , microbiology and biotechnology , pharmacology , biochemistry
Interest in GPCR ligand bias has increased in recent years due to evidence that positive and negative aspects of drug activity can be due to differential pathway signaling. As a result it is possible to develop drugs with reduced side effects by enhancing positive effects by favoring one pathway over another. The availability of assays that can measuring signaling events such as calcium mobilization, cAMP modulation, arrestin recruitment and receptor internalization has provided to opportunity to examine specific pathways. Here we provide examples of ligand bias and how quantification of receptor potency and efficacy in different pathways can be used to generate a ligand bias index.