G-protein coupled receptors bivalent ligands and drug design

G-protein coupled receptors (GPCR) represent a large family of receptors, w hich have been and still are targets of choice for drug discovery. Among th e different tools offered to medicinal chemists to design potent and select ive GPCR agonists or antagonists, the bivalent-ligand approach (which consi sts of bridging two pharmacophores in a single ligand) has proven to be, in many cases, valuable to improve potency, selectivity, intrinsic activity a nd in vivo profile of the corresponding monomer. This review will focus on GPCR ligands in drug research with particular emphasis on the most recent p rogress in the field.