title: Retinal dynamics underlie its switch from inverse agonist to agonist during rhodopsin activation.
abstract: X-ray and magnetic resonance approaches, though central to studies of G protein-coupled receptor (GPCR)-mediated signaling, cannot address GPCR protein dynamics or plasticity. Here we show that solid-state (2)H NMR relaxation elucidates picosecond-to-nanosecond-timescale motions of the retinal ligand that influence larger-scale functional dynamics of rhodopsin in membranes. We propose a multiscale activation mechanism whereby retinal initiates collective helix fluctuations in the meta I-meta II equilibrium on the microsecond-to-millisecond timescale.
authors.affiliation: Department of Chemistry, University of Arizona, Tucson, AZ, USA.
authors.forename: Andrey V
authors.initials: AV
authors.lastname: Struts
authors.forename: Gilmar F J
authors.initials: GF
authors.lastname: Salgado
authors.forename: Karina
authors.initials: K
authors.lastname: Martínez-Mayorga
authors.forename: Michael F
authors.initials: MF
authors.lastname: Brown
mesh_terms: D000818:Animals; D002417:Cattle; D008958:Models, Molecular; D019906:Nuclear Magnetic Resonance, Biomolecular; D011485:Protein Binding; D011487:Protein Conformation; D012172:Retinaldehyde / Q000737:chemistry / Q000378:metabolism*; D012243:Rhodopsin / Q000737:chemistry / Q000378:metabolism*
chemical_list: D012243:Rhodopsin; D012172:Retinaldehyde