Bitopic ligands: all-in-one orthosteric and allosteric.
Natural ligands of G-protein-coupled receptors interact with the orthosteric ligand binding site, as do most of the classical synthetic ligands. The discovery of ligands targeting different, allosteric binding sites considerably expanded the repertoire of G-protein-coupled receptor ligands. More recently, bitopic ligands have been described that target both orthosteric and allosteric sites at the same time.
Kamal
Maud
M
Institut Cochin, Université Paris Descartes, CNRS (UMR 8104), Paris, France.
Jockers
Ralf
R