Quantifying Signaling Bias: A Simple Approach to Quantify
Functional Selectivity and Agonist Bias
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Interest in GPCR ligand bias has increased in recent years due to evidence that positive and negative aspects of drug activity can be driven by differential pathway signaling. As a result it is possible to develop drugs with reduced side effects that enhance positive effects through favoring one pathway over another. The availability of assays that can measure signaling events such as calcium mobilization, cAMP modulation, arrestin recruitment and receptor internalization provides to ability to characterize compound action in multiple 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.