[GPCRs heterodimerization: a new way towards the discovery of function for the orphan receptors?].
G protein-coupled receptors (GPCRs), also called seven transmembrane domain (7TM) proteins, represent the largest family of cell surface receptors. GPCRs control a variety of physiological processes, are involved in multiple diseases and are major drug targets. Despite a vast effort of academic and industrial research, more than one hundred receptors remain orphans. These orphan GPCRs offer a great potential for drug discovery, as almost 60% of currently prescribed drugs target GPCRs. Deorphenization strategies have concentrated mainly on the identification of the natural ligands of these proteins. Recent advances have shown that orphan GPCRs, similar to orphan nuclear receptors, can regulate the function of non-orphan receptors by heterodimerization. These findings not only help to better understand the extraordinary diversity of GPCRs, but also open new perspectives for the identification of the function of these orphan receptors that hold great therapeutic potential.
Levoye
Angélique
A
Institut Pasteur, Laboratoire de Pathogénie Virale Moléculaire, INSERM U819, Département de Virologie, 28, rue du Docteur Roux, 75724, Paris, France. levoye@pasteur.fr
Jockers
Ralf
R
D000818:Animals; D019281:Dimerization; D006801:Humans; D008958:Models, Molecular; D011487:Protein Conformation; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry / Q000502:physiology*
D043562:Receptors, G-Protein-Coupled