G-protein coupled receptors bivalent ligands and drug design

Abstract

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

• agonist
• antagonist
• bivalent ligands
• G-protein coupled receptor