Topic: allosteric modulation

Drug responses reflect both a ligand’s intrinsic properties and the sensitivity of the biological assay. Receptor abundance and signal-transduction efficiency can therefore alter observed activity and complicate translation from laboratory assays to living systems. Terry Kenakin examines controlled changes in system sensitivity as a way to distinguish the underlying properties of GPCR ligands. Adjusting receptor density and cellular responsiveness permits affinity and efficacy to be assessed within a common operational framework. Lower sensitivity can reveal partial agonism and support estima