Abstract

G protein-coupled receptors represent one of the largest families of drug targets. Time and cost may be saved if GPCR modulators are assessed in terms of signaling pathway selectivity, species selectivity, and selectivity against closely-related family members early in the drug discovery process, perhaps even at the stage of high-throughput screening. Examples are given of how these kinds of selectivity have been addressed during screening.

Keywords: β-Arrestin, desensitization, G protein-coupled receptor, selectivity, G protein, high throughput screening, receptor subtype, species, Arrestin, 2-adrenergic receptor, (hydroxyphenylorciprenaline), GPCR signaling, MAPKs, angiotensin II receptor type 1, parathy-roid hormone receptor, protease activated receptor, vasopressin 2 receptor, herkinorin, Ligand Pharmaceutical's Encoded Combinatorial Librar-ies on Polymeric Support, bradykinin receptor 1, melano-cortin (MC)-4 receptor (MC4R)