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Published Online October 25, 2007
Science DOI: 10.1126/science.1150577

Research Articles

Submitted on September 17, 2007
Accepted on October 11, 2007

High-Resolution Crystal Structure of an Engineered Human {beta}2-Adrenergic G Protein–Coupled Receptor

Vadim Cherezov 1{dagger}, Daniel M. Rosenbaum 2{dagger}, Michael A. Hanson 1, Søren G. F. Rasmussen 3, Foon Sun Thian 3, Tong Sun Kobilka 3, Hee-Jung Choi 4, Peter Kuhn 5, William I. Weis 4, Brian K. Kobilka 3*, Raymond C. Stevens 1*

1 Department of Molecular Biology, Scripps Research Institute, La Jolla, CA 92037, USA.
2 Department of Molecular and Cellular Physiology, Stanford University School of Medicine, Stanford, CA 94305, USA.; These authors contributed equally to this work.
3 Department of Molecular and Cellular Physiology, Stanford University School of Medicine, Stanford, CA 94305, USA.
4 Department of Molecular and Cellular Physiology, Stanford University School of Medicine, Stanford, CA 94305, USA.; Department of Structural Biology, Stanford University School of Medicine, Stanford, CA 94305, USA.
5 Department of Cell Biology, Scripps Research Institute, La Jolla, CA 92037, USA.

* To whom correspondence should be addressed.
Brian K. Kobilka , E-mail: kobilka{at}stanford.edu
Raymond C. Stevens , E-mail: stevens{at}scripps.edu

{dagger}These authors contributed equally to this work.

G protein–coupled receptors comprise the largest family of eukaryotic signal transduction proteins that communicate across the membrane. We report the crystal structure of a human {beta}2-adrenergic receptor–T4 lysozyme fusion protein bound to the partial inverse agonist carazolol at 2.4 Å resolution. The structure provides a high-resolution view of a human G protein–coupled receptor bound to a diffusible ligand. Ligand-binding site accessibility is enabled by the second extracellular loop which is held out of the binding cavity by a pair of closely spaced disulfide bridges and a short helical segment within the loop. Cholesterol, a necessary component for crystallization, mediates an intriguing parallel association of receptor molecules in the crystal lattice. Although the location of carazolol in the {beta}2-adrenergic receptor is very similar to that of retinal in rhodopsin, structural differences in the ligand binding site and other regions highlight the challenges in using rhodopsin as a template model for this large receptor family.


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A. K. Shukla, J.-P. Sun, and R. J. Lefkowitz (2008)
Mol. Pharmacol. 73, 1333-1338
   Abstract »    Full Text »    PDF »
Two Amino Acid Substitutions within the First External Loop of CCR5 Induce Human Immunodeficiency Virus-Blocking Antibodies in Mice and Chickens.
C. Pastori, A. Clivio, L. Diomede, R. Consonni, G. M. S. De Mori, R. Longhi, G. Colombo, and L. Lopalco (2008)
J. Virol. 82, 4125-4134
   Abstract »    Full Text »    PDF »
Highlights From The Literature.
(2008)
Physiology 23, 61-63
   Full Text »    PDF »
Role of {beta}-Adrenoceptor Signaling in Skeletal Muscle: Implications for Muscle Wasting and Disease.
G. S. Lynch and J. G. Ryall (2008)
Physiol Rev 88, 729-767
   Abstract »    Full Text »    PDF »
Wide Turn Diversity in Protein Transmembrane Helices Implications for G-Protein-Coupled Receptor and Other Polytopic Membrane Protein Structure and Function.
R. P. Riek, A. A. Finch, G. E. Begg, and R. M. Graham (2008)
Mol. Pharmacol. 73, 1092-1104
   Abstract »    Full Text »    PDF »
Structure of the Complement Factor 5a Receptor-Ligand Complex Studied by Disulfide Trapping and Molecular Modeling.
I. S. Hagemann, D. L. Miller, J. M. Klco, G. V. Nikiforovich, and T. J. Baranski (2008)
J. Biol. Chem. 283, 7763-7775
   Abstract »    Full Text »    PDF »
Multiple Roles for the C-terminal Tail of the Chemokine Scavenger D6.
C. V. McCulloch, V. Morrow, S. Milasta, I. Comerford, G. Milligan, G. J. Graham, N. W. Isaacs, and R. J. B. Nibbs (2008)
J. Biol. Chem. 283, 7972-7982
   Abstract »    Full Text »    PDF »
Dimerization and oligomerization of G-protein-coupled receptors: debated structures with established and emerging functions.
L. Szidonya, M. Cserzo, and L. Hunyady (2008)
J. Endocrinol. 196, 435-453
   Abstract »    Full Text »    PDF »
Vertebrate Membrane Proteins: Structure, Function, and Insights from Biophysical Approaches.
D. J. Muller, N. Wu, and K. Palczewski (2008)
Pharmacol. Rev. 60, 43-78
   Abstract »    Full Text »    PDF »
Conformational thermostabilization of the {beta}1-adrenergic receptor in a detergent-resistant form.
M. J. Serrano-Vega, F. Magnani, Y. Shibata, and C. G. Tate (2008)
PNAS 105, 877-882
   Abstract »    Full Text »    PDF »
Site-specific Incorporation of Keto Amino Acids into Functional G Protein-coupled Receptors Using Unnatural Amino Acid Mutagenesis.
S. Ye, C. Kohrer, T. Huber, M. Kazmi, P. Sachdev, E. C.Y. Yan, A. Bhagat, U. L. RajBhandary, and T. P. Sakmar (2008)
J. Biol. Chem. 283, 1525-1533
   Abstract »    Full Text »    PDF »
GPCR Engineering Yields High-Resolution Structural Insights into 2-Adrenergic Receptor Function.
D. M. Rosenbaum, V. Cherezov, M. A. Hanson, S. G. F. Rasmussen, F. S. Thian, T. S. Kobilka, H.-J. Choi, X.-J. Yao, W. I. Weis, R. C. Stevens, et al. (2007)
Science 318, 1266-1273
   Abstract »    Full Text »    PDF »


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