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

@article{Conn2009AllostericMO,
  title={Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders},
  author={Peter Jeffrey Conn and Arthur Christopoulos and Craig W Linsdley},
  journal={Nature Reviews Drug Discovery},
  year={2009},
  volume={8},
  pages={41-54}
}
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… CONTINUE READING
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