Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders

Peter Jeffrey Conn, Arthur Christopoulos, Craig W Lindsley

Research output: Contribution to journalArticleResearchpeer-review

731 Citations (Scopus)


Despite G-protein-coupled receptors (GPCRs) being among the most fruitful targets for marketed drugs, intense discovery efforts for several GPCR subtypes have failed to deliver selective drug candidates. Historically, drug discovery programmes for GPCR ligands have been dominated by efforts to develop agonists and antagonists that act at orthosteric sites for endogenous ligands. However, in recent years, there have been tremendous advances in the discovery of novel ligands for GPCRs that act at allosteric sites to regulate receptor function. These compounds provide high selectivity, novel modes of efficacy and may lead to novel therapeutic agents for the treatment of multiple psychiatric and neurological human disorders.
Original languageEnglish
Pages (from-to)41 - 54
Number of pages14
JournalNature Reviews Drug Discovery
Issue number1
Publication statusPublished - 2009

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