title: Relationship between homo-oligomerization of a mammalian olfactory receptor and its activation state demonstrated by bioluminescence resonance energy transfer.
abstract: G-protein-coupled receptor homo-oligomerization has been increasingly reported. However, little is known regarding the relationship between activation of the receptor and its association/conformational states. The mammalian olfactory receptors (ORs) belong to the G protein-coupled receptor superfamily. In this study, the homo-oligomerization status of the human OR1740 receptor and its involvement in receptor activation upon odorant ligand binding were addressed by co-immunoprecipitation and bioluminescence resonance energy transfer approaches using crude membranes or membranes from different cellular compartments. For the first time, our data clearly show that mammalian ORs constitutively self-associate into homodimers at the plasma membrane level. This study also demonstrates that ligand binding mediates a conformational change and promotes an inactive state of the OR dimers at high ligand concentrations. These findings support and validate our previously proposed model of OR activation/inactivation based on the tripartite odorant-binding protein-odorant-OR partnership.
authors: UR1197 Neurobiologie de l'Olfaction et Modélisation en Imagerie, Institut National de la Recherche Agronomique, Domaine de Vilvert, F-78350 Jouy-en-Josas, France.
authors: Fallou
authors: F
authors: Wade
authors: Agathe
authors: A
authors: Espagne
authors: Marie-Annick
authors: MA
authors: Persuy
authors: Jasmina
authors: J
authors: Vidic
authors: Régine
authors: R
authors: Monnerie
authors: Fabienne
authors: F
authors: Merola
authors: Edith
authors: E
authors: Pajot-Augy
authors: Guenhaël
authors: G
authors: Sanz
mesh_terms: D004735:Energy Transfer; D006801:Humans; D008163:Luminescent Measurements; D011485:Protein Binding; D011487:Protein Conformation; D055503:Protein Multimerization; D018035:Receptors, Odorant / Q000737:chemistry / Q000378:metabolism*
chemical_list: D018035:Receptors, Odorant; C045648:odorant-binding protein