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Science 1 November 1996:
Vol. 274. no. 5288, pp. 768 - 770
DOI: 10.1126/science.274.5288.768
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Reports

Requirement of Rigid-Body Motion of Transmembrane Helices for Light Activation of Rhodopsin

David L. Farrens, * Christian Altenbach, Ke Yang, dagger Wayne L. Hubbell, ddagger H. Gobind Khorana ddagger

Conformational changes are thought to underlie the activation of heterotrimeric GTP-binding protein (G protein)-coupled receptors. Such changes in rhodopsin were explored by construction of double cysteine mutants, each containing one cysteine at the cytoplasmic end of helix C and one cysteine at various positions in the cytoplasmic end of helix F. Magnetic dipolar interactions between spin labels attached to these residues revealed their proximity, and changes in their interaction upon rhodopsin light activation suggested a rigid body movement of helices relative to one another. Disulfide cross-linking of the helices prevented activation of transducin, which suggests the importance of this movement for activation of rhodopsin.

D. L. Farrens, K. Yang, H. G. Khorana, Departments of Biology and Chemistry, Massachusetts Institute of Technology, Cambridge, MA 02139, USA.
C. Altenbach and W. L. Hubbell, Jules Stein Eye Institute and Department of Chemistry, University of California, Los Angeles, CA 90095-7008, USA.
*   Present address: Department of Biochemistry and Molecular Biology, Oregon Health Sciences University, Portland, OR 97201, USA.

dagger    Present address: Memorial Sloan-Kettering Cancer Center, 1275 York Avenue, New York, NY 10021, USA.

ddagger    To whom correspondence should be addressed.

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A Naturally Occurring Mutation of the Opsin Gene (T4R) in Dogs Affects Glycosylation and Stability of the G Protein-coupled Receptor.
L. Zhu, G.-F. Jang, B. Jastrzebska, S. Filipek, S. E. Pearce-Kelling, G. D. Aguirre, R. E. Stenkamp, G. M. Acland, and K. Palczewski (2004)
J. Biol. Chem. 279, 53828-53839
   Abstract »    Full Text »    PDF »
Conformational Changes in the Phosphorylated C-terminal Domain of Rhodopsin during Rhodopsin Arrestin Interactions.
O. G. Kisselev, M. A. Downs, J. H. McDowell, and P. A. Hargrave (2004)
J. Biol. Chem. 279, 51203-51207
   Abstract »    Full Text »    PDF »
Analysis of the Third Transmembrane Domain of the Human Type 1 Angiotensin II Receptor by Cysteine Scanning Mutagenesis.
S. S. Martin, A. A. Boucard, M. Clement, E. Escher, R. Leduc, and G. Guillemette (2004)
J. Biol. Chem. 279, 51415-51423
   Abstract »    Full Text »    PDF »
Structural Mimicry in Class A G Protein-coupled Receptor Rotamer Toggle Switches: THE IMPORTANCE OF THE F3.36(201)/W6.48(357) INTERACTION IN CANNABINOID CB1 RECEPTOR ACTIVATION.
S. D. McAllister, D. P. Hurst, J. Barnett-Norris, D. Lynch, P. H. Reggio, and M. E. Abood (2004)
J. Biol. Chem. 279, 48024-48037
   Abstract »    Full Text »    PDF »
The Hydrodynamic Properties of Dark- and Light-activated States of n-Dodecyl {beta}-D-Maltoside-solubilized Bovine Rhodopsin Support the Dimeric Structure of Both Conformations.
R. Medina, D. Perdomo, and J. Bubis (2004)
J. Biol. Chem. 279, 39565-39573
   Abstract »    Full Text »    PDF »
"Induced-Fit" Mechanism for Catecholamine Binding to the {beta}2-Adrenergic Receptor.
R. Del Carmine, P. Molinari, M. Sbraccia, C. Ambrosio, and T. Costa (2004)
Mol. Pharmacol. 66, 356-363
   Abstract »    Full Text »    PDF »
Modulation of Ligand Selectivity Associated with Activation of the Transmembrane Region of the Human Follitropin Receptor.
L. Montanelli, J. J. J. Van Durme, G. Smits, M. Bonomi, P. Rodien, E. J. Devor, K. Moffat-Wilson, L. Pardo, G. Vassart, and S. Costagliola (2004)
Mol. Endocrinol. 18, 2061-2073
   Abstract »    Full Text »    PDF »
Preferential Formation of MT1/MT2 Melatonin Receptor Heterodimers with Distinct Ligand Interaction Properties Compared with MT2 Homodimers.
M. A. Ayoub, A. Levoye, P. Delagrange, and R. Jockers (2004)
Mol. Pharmacol. 66, 312-321
   Abstract »    Full Text »    PDF »
Rhodopsin Activation Exposes a Key Hydrophobic Binding Site for the Transducin {alpha}-Subunit C Terminus.
J. M. Janz and D. L. Farrens (2004)
J. Biol. Chem. 279, 29767-29773
   Abstract »    Full Text »    PDF »
Coupling of retinal isomerization to the activation of rhodopsin.
A. B. Patel, E. Crocker, M. Eilers, A. Hirshfeld, M. Sheves, and S. O. Smith (2004)
PNAS 101, 10048-10053
   Abstract »    Full Text »    PDF »
Synergistic Contributions of the Functional Groups of Epinephrine to Its Affinity and Efficacy at the {beta}2 Adrenergic Receptor.
G. Liapakis, W. C. Chan, M. Papadokostaki, and J. A. Javitch (2004)
Mol. Pharmacol. 65, 1181-1190
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Different Structural States of the Proteolipid Membrane Are Produced by Ligand Binding to the Human {delta}-Opioid Receptor as Shown by Plasmon-Waveguide Resonance Spectroscopy.
I. D. Alves, S. M. Cowell, Z. Salamon, S. Devanathan, G. Tollin, and V. J. Hruby (2004)
Mol. Pharmacol. 65, 1248-1257
   Abstract »    Full Text »
Gonadotropin-Releasing Hormone Receptors.
R. P. Millar, Z.-L. Lu, A. J. Pawson, C. A. Flanagan, K. Morgan, and S. R. Maudsley (2004)
Endocr. Rev. 25, 235-275
   Abstract »    Full Text »    PDF »
Evolutionary Trace of G Protein-coupled Receptors Reveals Clusters of Residues That Determine Global and Class-specific Functions.
S. Madabushi, A. K. Gross, A. Philippi, E. C. Meng, T. G. Wensel, and O. Lichtarge (2004)
J. Biol. Chem. 279, 8126-8132
   Abstract »    Full Text »    PDF »
Vertebrate ultraviolet visual pigments: Protonation of the retinylidene Schiff base and a counterion switch during photoactivation.
A. K. Kusnetzow, A. Dukkipati, K. R. Babu, L. Ramos, B. E. Knox, and R. R. Birge (2004)
PNAS 101, 941-946
   Abstract »    Full Text »    PDF »
Locking the Dimeric GABAB G-Protein-Coupled Receptor in Its Active State.
J. Kniazeff, P.-P. Saintot, C. Goudet, J. Liu, A. Charnet, G. Guillon, and J.-P. Pin (2004)
J. Neurosci. 24, 370-377
   Abstract »    Full Text »    PDF »
Sequential Binding of Agonists to the {beta}2 Adrenoceptor: KINETIC EVIDENCE FOR INTERMEDIATE CONFORMATIONAL STATES.
G. Swaminath, Y. Xiang, T. W. Lee, J. Steenhuis, C. Parnot, and B. K. Kobilka (2004)
J. Biol. Chem. 279, 686-691
   Abstract »    Full Text »    PDF »
The Three-dimensional Structure of Bovine Rhodopsin Determined by Electron Cryomicroscopy.
A. Krebs, P. C. Edwards, C. Villa, J. Li, and G. F. X. Schertler (2003)
J. Biol. Chem. 278, 50217-50225
   Abstract »    Full Text »    PDF »
Insights into G Protein Structure, Function, and Regulation.
T. M. Cabrera-Vera, J. Vanhauwe, T. O. Thomas, M. Medkova, A. Preininger, M. R. Mazzoni, and H. E. Hamm (2003)
Endocr. Rev. 24, 765-781
   Abstract »    Full Text »    PDF »
Organization and Functions of Interacting Domains for Signaling by Protein-Protein Interactions.
E. Buck and R. Iyengar (2003)
Sci. STKE 2003, re14
   Abstract »    Full Text »    PDF »
Mutational Analysis and Molecular Modeling of the Binding Pocket of the Metabotropic Glutamate 5 Receptor Negative Modulator 2-Methyl-6-(phenylethynyl)-pyridine.
P. Malherbe, N. Kratochwil, M.-T. Zenner, J. Piussi, C. Diener, C. Kratzeisen, C. Fischer, and R. H. P. Porter (2003)
Mol. Pharmacol. 64, 823-832
   Abstract »    Full Text »    PDF »
Rhodopsin Determinants for Transducin Activation: A GAIN-OF-FUNCTION APPROACH.
M. Natochin, K. G. Gasimov, M. Moussaif, and N. O. Artemyev (2003)
J. Biol. Chem. 278, 37574-37581
   Abstract »    Full Text »    PDF »
Constitutive Activation of CCR5 and CCR2 Induced by Conformational Changes in the Conserved TXP Motif in Transmembrane Helix 2.
D. A. Arias, J.-M. Navenot, W.-b. Zhang, J. Broach, and S. C. Peiper (2003)
J. Biol. Chem. 278, 36513-36521
   Abstract »    Full Text »    PDF »


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