BIASED LIGANDS AND METHODS OF IDENTIFYING SAME

摘要

The present invention relates to G protein-coupled receptor ligands having a relative efficacy for stimulating ß-arrestin/G protein-coupled receptor kinase (GRK) function (e.g., signaling) that is greater than their relative efficacy for stimulating G-protein signaling function. These "ß-arrestin/GRK biased ligands" can act as agonists or antagonists of G protein-mediated signaling and agonists of ß-arrestin/GRK-mediated signal transduction. The invention further relates to methods of identifying such ligands and to methods of using same in a variety of therapeutic settings.