Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders.

Conn PJ, Lindsley CW, Meiler J, Niswender CM
Nat Rev Drug Discov. 2014 13 (9): 692-708

PMID: 25176435 · PMCID: PMC4208620 · DOI:10.1038/nrd4308

Novel allosteric modulators of G protein-coupled receptors (GPCRs) are providing fundamental advances in the development of GPCR ligands with high subtype selectivity and novel modes of efficacy that have not been possible with traditional approaches. As new allosteric modulators are advancing as drug candidates, we are developing an increased understanding of the major advantages and broad range of activities that can be achieved with these agents through selective modulation of specific signalling pathways, differential effects on GPCR homodimers versus heterodimers, and other properties. This understanding creates exciting opportunities, as well as unique challenges, in the optimization of novel therapeutic agents for disorders of the central nervous system.

MeSH Terms (8)

Allosteric Regulation Animals Central Nervous System Agents Central Nervous System Diseases Drug Discovery Humans Receptors, G-Protein-Coupled Treatment Outcome

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