De-Orphanizing GPCRs and Drug Development

Abstract

Traditionally, the family of G protein-coupled receptors (GPCRs) has been divided into “classical” GPCRs and olfactory (or gustatory) GPCRs. The classical GPCRs comprise receptors for all neurotransmitters and hormones, displaying a vast chemical diversity among their natural ligands. Odorant receptors are believed to bind volatile molecules, but the mechanisms of ligand binding in this group are less well-understood.