Development of functionally selective agonists as novel therapeutic agents

Traditionally, drug selectivity has been attributed solely to differential affinity for different receptor subtypes. Recent experimental evidence suggests that, in addition to receptor subtype selectivity, drugs may be selective for individual signaling pathways coupled to a single receptor subtype. This ‘functional selectivity’ holds the promise of improved therapeutic selectivity and reduced adverse effects.

Section editors:David Sibley – National Institute of Neurological Disorders and Stroke, National Institutes of Health, Bethesda, USAC. Anthony Altar – Psychiatric Genomics, Gaithersburg, USATheresa Branchek – Lundbeck Research, Paramus, USA