G protein-coupled receptors (GPCRs) are highly successful drug targets, particularly for central nervous system (CNS) disorders. Compared to traditional drugs that target the orthosteric ligand-binding site of GPCRs, allosteric modulators have the potential to achieve greater subtype selectivity and allow the normal function of endogenous ligands to be preserved. Conn and colleagues reflect on the key principles for successful optimization of GPCR allosteric modulators.
- P. Jeffrey Conn
- Craig W. Lindsley
- Colleen M. Niswender
