The best of both worlds? Bitopic orthosteric/allosteric ligands of g protein-coupled receptors.

@article{Valant2012TheBO,
  title={The best of both worlds? Bitopic orthosteric/allosteric ligands of g protein-coupled receptors.},
  author={C{\'e}line Valant and J Robert Lane and Patrick M. Sexton and Arthur Christopoulos},
  journal={Annual review of pharmacology and toxicology},
  year={2012},
  volume={52},
  pages={153-78}
}
It is now acknowledged that G protein-coupled receptors, the largest class of drug targets, adopt multiple active states that can be preferentially stabilized by orthosteric ligands or allosteric modulators, thus giving rise to the phenomenon of pathway-biased signaling. In the past few years, researchers have begun to explore the potential of linking orthosteric and allosteric pharmacophores to yield bitopic hybrid ligands. This approach is an extension of the more traditional bivalent ligand… CONTINUE READING