Selected Publications
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Lin, S., Gether, U. and Kobilka, B.K. Ligand stabilization of the beta 2 adrenergic receptor: Effect of DTT on receptor conformation monitored by circular dichroism and fluorescence spectroscopy . Biochemistry, 1996. 35: p. 14445-51. |
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Gether, U., Lin, S., Ghanouni, P., Ballesteros, J.A., Weinstein, H., and Kobilka, B.K. Agonists induce conformational changes in transmembrane domains III and VI of the beta2 adrenoceptor. Embo J, 1997. 16(22): p. 6737-47. |
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Gether, U. and Kobilka, B.K. G Protein-coupled Receptors: Mechanism of Agonist activation. J. Biol. Chem. 1997. 273: p. 17979-82. |
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Seifert, R., Wenzel-Seifert, K., Lee, T.W., Gether, U., Sanders-Bush, E., and Kobilka, B.K. Different effects of Gsa splice variants on beta2-adrenoreceptor-mediated signaling. The beta2-adrenoreceptor coupled to the long splice variant of Gsa has properties of a constitutively active receptor. J Biol Chem, 1998. 273(9): p. 5109-16. |
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Lee, T.W., R. Seifert, X. Guan, and B.K. Kobilka, Restricting the mobility of Gs alpha: impact on receptor and effector coupling. Biochemistry, 1999. 38(42): p. 13801-9. |
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Chruscinski, A.J., Rohrer, D.K., Schauble, E., Desai, K.H., Bernstein, D., and Kobilka, B.K. Targeted disruption of the beta2 adrenergic receptor gene. J Biol Chem, 1999. 274(24): p. 16694-700. |
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Rohrer, D.K., Chruscinski, A., Schauble, E.H., Bernstein, D., and Kobilka, B.K. Cardiovascular and metabolic alterations in mice lacking both beta1- and beta2-adrenergic receptors. J Biol Chem, 1999. 274(24): p. 16701-8. |
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Altman, J.D., Trendelenburg, A.U., MacMillan, L., Bernstein, D., Limbird, L., Starke, K., Kobilka, B.K., and Hein, L. Abnormal regulation of the sympathetic nervous system in alpha2A- adrenergic receptor knockout mice. Mol Pharmacol, 1999. 56(1): p. 154-61. |
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Winder, D.G., Martin, K.C., Muzzio, I.A., Rohrer, D., Chruscinski, A., Kobilka, B. and Kandel, E.R., ERK plays a regulatory role in induction of LTP by theta frequency stimulation and its modulation by beta-adrenergic receptors. Neuron, 1999. 24(3): p. 715-26. |
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Hein, L., Altman, J.D., and Kobilka, B.K. Two functionally distinct alpha2-adrenergic receptors regulate sympathetic neurotransmission. Nature, 1999. 402(6758): p. 181-4. |
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Ghanouni, P., Schambye, H., Seifert, R., Lee, T.W., Rasmussen, S.G., Gether, U., and Kobilka, B.K. The Effect of pH on beta2 Adrenoceptor Function. Evidence for protonation-dependent activation. J Biol Chem, 2000. 275(5): p. 3121-3127. |
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Hurt, C.M., Feng, F. Y., and Kobilka, B. K. Cell-Type Specific Targeting of the Alpha2C Adrenoceptor: Evidence for the organization of receptor microdomains during neuronal differentiation of PC12 cells. J Biol Chem, 2000. 275: p. 35424-31. |
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Ghanouni, P., Steenhuis, J.J., Farrens, D.L., and Kobilka, B.K., Agonist-induced conformational changes in the G protein coupling domain of the beta 2 adrenergic receptor. Proc Natl Acad Sci U S A, 2001. 98(11):p.5997-6002. |
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Ghanouni, P., Gryczynski, Z., Steenhuis, J.J., Lee, T.W., Farrens, D.L., Lakowicz, J.R., and Kobilka, B.K. Functionally different agonists induce distinct conformations in the G protein coupling domain of the beta 2 adrenergic receptor. J Biol Chem, 2001. 276(27):p. 24433-6. |
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Peleg, G., Ghanouni, P., Kobilka, B.K., and Zare, R.N. Single-molecule spectroscopy of the beta 2 adrenergic receptor: Observation of conformational substates in a membrane protein. Proc Natl Acad Sci U S A, 2001. 98:p.8469-74. |
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Devic, E., Xiang, Y., Gould, D., and Kobilka, B.K. Beta adrenergic receptor subtype-specific signaling in cardiac myoctyes from beta 1 and beta 2 adrenoceptor knockout mice. Mol Pharmacol, 2001. 60(3):p. 577-83. |
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Swaminath, G., Steenhuis, J.J., Kobilka, B.K., and Lee, T.W. Allosteric modulation of the beta 2 adrenergic receptor by Zn2+. Mol Pharmacol, 2002, 61: p. 65-72. |
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Xiang, Y., Rybin, V.O., S. Steinberg, S.S. and Kobilka, B.K. Caveolar localization dictates physiologic signaling of beta2 adrenoceptors in neonatal cardiac myocytes. J. Biol. Chem., 2002. 277(37): p. 34280-6. |
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Xiang, Y., Devic, E., and Kobilka, B.K. The PDZ binding motif of the beta1 adrenergic receptor modulates receptor trafficking and signaling in cardiac myocytes. J.Biol. Chem., 2002. 277(37): p. 33783-90. |
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Neumann, L., T. Wohland, R.J. Whelan, R.N. Zare, and B.K. Kobilka, Functional immobilization of a ligand-activated G-protein-coupled receptor. Chembiochem, 2002. 3(10): p. 993-8. |
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Brum, P.C., J. Kosek, A. Patterson, D. Bernstein, and B. Kobilka, Abnormal cardiac function associated with sympathetic nervous system hyperactivity in mice. Am J Physiol Heart Circ Physiol, 2002. 283(5): p. H1838-45.. |
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Swaminath, G., T.W. Lee, and B. Kobilka, Identification of an allosteric binding site for Zn2+ on the Beta 2 adrenergic receptor. J Biol Chem, 2003. 278(1): p. 352-6. |
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Y. Xiang and B. Kobilka, Myocyte Adrenoceptor Signaling Pathways. Science, 2003. 300: p 1530-1532. |
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Y. Xiang and B. Kobilka, The PDZ-binding motif of the beta 2 adrenoceptor is essential for physiologic signaling and trafficking in cardiac myocytes. PNAS, 2003. 100: p 10776-10781. |
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Swaminath, G., Y. Xiang, T.W. Lee, J. Steenhuis, C. Parnot and B. Kobilka, Sequential Binding of Agonists to the beta 2 Adrenoceptor: Kinetic Evidence for Intermediate Conformational States. J Biol Chem, 2004. 279(1): p. 686-691. |
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Devanathan, S., Yao, Z., Salamon, Z., Kobilka, B.K., and Tollin, G.. Plasmon-waveguide resonance studies of ligand binding to the human Beta2-adrenergic receptor. Biochemistry, 2004.43:3280-8. |
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Kobilka,
B.K. Agonist binding: a multistep process. Mol Pharmacol. 2004 May;65(5):1060-2. |
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Parnot, C. and Kobilka, B.K. Toward understanding GPCR dimers. Nat Struct Mol Biol. 2004 Aug;11(8):691-2. |
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Xiang, Y., Naro, F., Zoudilova, M., Jin, S.L, Conti, M., and Kobilka, B.K. PDE4D is required for Beta2AR subtype-specific signaling in cardiac myocytes. Proc Natl Acad Sci U S A, 2005. 102(3): p. 909-14. |
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Swaminath, G., Deupi, X., Lee, T.W., Zhu, W., Thian, F.S., Kobilka, T.S. and Kobilka, B.K. Probing the Beta2 adrenoceptor binding site with catechol reveals differences in binding and activation by agonists and partial agonists. J. Biol. Chem., 2005. 280, 22165-71. |
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Trester-Zedlitz, M., Burlingame, A., Kobilka, B. K., von Zastrow, M. Mass Spectrometric Analysis of Agonist Effects on Posttranslational Modifications of the beta-2 Adrenoceptor in Mammalian Cells. Biochemistry, 2005. 44, 6133-43. |
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Yao, X., Parnot, C., Deupi, X., Ratnala, V.R., Swaminath, G., Farrens, D., and Kobilka, B., Coupling ligand structure to specific conformational switches in the beta(2)-adrenoceptor. Nat Chem Biol, 2006. 2(8): p. 417-22. |
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Shcherbakova, O.G., C.M. Hurt, Y. Xiang, M.L. Dell'acqua, Q. Zhang, R.W. Tsien, and B.K. Kobilka, Organization of beta-adrenoceptor signaling compartments by sympathetic innervation of cardiac myocytes. J Cell Biol, 2007. 176(4): p. 521-33. |
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Whorton, M.R., M.P. Bokoch, S.G. Rasmussen, B. Huang, R.N. Zare, B. Kobilka, and R.K. Sunahara, A monomeric G protein-coupled receptor isolated in a high-density lipoprotein particle efficiently activates its G protein. Proc Natl Acad Sci USA, 2007. 104(18): p. 7682-7. |
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Kobilka, B.K. and Deupi, X., Conformational complexity of G-protein-coupled receptors. Trends Pharmacol Sci, 2007. 28(8): p. 397-406. |
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Granier, S., S. Kim, A.M. Shafer, V.R. Ratnala, J.J. Fung, R.N. Zare, and B. Kobilka, Structure and conformational changes in the C-terminal domain of the beta2-adrenoceptor: insights from fluorescence resonance energy transfer studies. J Biol Chem, 2007. 282(18): p. 13895-905. |
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Kobilka, B.K. and Deupi, X., Conformational complexity of G-protein-coupled receptors. Trends Pharmacol Sci, 2007. |
| Rasmussen, S.G.F, Choi, H.J, Rosenbaum, D.M., Kobilka, T.S., Thian, F.S., Edwards, P.C., Burghammer, M., Rratnala, V.R.P, Sanishvili, R. Fischetti, R.F., Schertler, G.F.X, Weis, W.I., Kobilka, B.K ., Crystal structure of the human beta 2 adrenergic G protein coupled receptor. Nature, 2007. 450:383-7. | |
| Day, P. W., Rasmussen, S.G.F, Parnot, C., Fung, J.J., Masood, A., Kobilka, T.S., Yao, X.J., Choi, H.J, , Weis, W.I., Roher, D.K., Kobilka, B.K ., A monoclonal antibody for G protein-coupled receptor crystallography. Nature Methohds, 2007. 4:927-9. | |
| Rosenbaum, D.M, Cerezov, V., Hanson, M.A., Rasmussen, S.G.F., Thian, F.S., Kobilka, T.S., Choi, H.J., Yao, X.J., Weis, W.I., Stevens, R.C., Kobilka, B.K ., GPCR Engineering Yields High-Resolution Structural Insights into beta 2-Adrenergic Receptor Function. Science, 2007. 318:1266-1273. | |
| Cerezov, V., Rosenbaum, D.M, Hanson, M.A., Rasmussen, S.G.F., Thian, F.S., Kobilka, T.S., Choi, H.J., Kuhn, P., Weis, W.I., Kobilka, B.K ., Stevens, R.C., High-Resolution Crystal Structure of an Engineered Human beta 2-Adrenergic G Protein–Coupled Receptor. Science, 2007. 318:1258-1265. | |
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Kolb, P., Rosenbaum, D.M., Irwin, J.J., Fung, J.J., Kobilka, B.K., and Shoichet, B.K., Structure-based discovery of beta 2-adrenergic receptor ligands. Proc Natl Acad Sci U S A, 2009. 106(16): p. 6843-6848. |
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Yao, X.J., Vélez Ruiz, G., Whorton, M.R., Rasmussen, S.G.F., DeVree, B.T., Deupi, X., Sunahara, R.K., and Kobilka, B.K., The effect of ligand efficacy on the formation and stability of a GPCR-G protein complex. Proc Natl Acad Sci U S A, 2009. 106(23): p. 9501-9506. |
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Fung, J.J., Deupi, X., Pardo, L., Yao, X.J., Velez-Ruiz, G.A., DeVree, B., Sunahara, R.K., and Kobilka, B.K., Ligand regulated oligomerization of beta2-adrenoceptors in a model lipid bilayer. EMBO Journal, 2009. 28(21): p. 3315-28. |
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Rosenbaum, D.M., Rasmussen, S.G., Kobilka, B.K. The structure and function of G-protein-coupled receptors. Nature, 2009. 459(7245): 356-363. |
| Bokoch, M.P., Zou, Y., Rasmussen, S.G.F., Liu, C.W., Nygaard, R., Rosenbaum, D.M., Fung, J.J., Choi, H.J., Thian, F.S., Kobilka, T.S., Puglisi, J.D., Weis, W.I., Pardo, L., Prosser, R.S., Mueller, L., Kobilka, B.K. Ligand-specific regulation of the extracellular surface of a G protein coupled receptor. Nature, 2010. 463:p.108-112. | |
| Rosenbaum, D.M., Zhang, C., Lyons, J., Holl, R., Aragao, D., Arlow, D.H., Rasmussen, S.G.F., Choi, H.J., DeVree, B.T., Sunahara, R.K., Chae, P.S., Gellman, S.H., Dror, R., Shaw, D.E., Weis, W.I., Caffrey, M., Gmeiner, P., and Kobilka, B.K., Structure and Function of an Irreversible Agonist-β2 Adrenoceptor complex. Nature 469, 236-240 (2011). | |
| Rasmussen, S.G., Choi, H.J., Fung, J.J., Pardon, E., Casarosa, P., Chae, P.S., DeVree, B.T., Rosenbaum, D.M., Thian, F.S., Kobilka, T.S., Schanpp, A., Konetzki, I., Sunahara, R.K., Gellman, S.H., Pautsch, A., Steyaert, J., Weis, W.I., and Kobilka, B.K., Structure of a nanobody-stabilized active state of the β2 adrenoceptor. Nature 469, 175-180 (2011). | |
| Rasmussen, S.G., Devree, B.T., Zou, Y., Kruse, A.C., Chung, K.Y., Kobilka, T.S., Thian, F.S., Chae, P.S., Pardon, E., Calinski, D., Mathiesen, J.M., Shah, S.T., Lyons, J.A., Caffrey, M., Gellman, S.H., Steyaert, J., Skiniotis, G., Weis, W.I., Sunahara, R.K., and Kobilka, B.K., Crystal structure of the beta(2) adrenergic receptor-Gs protein complex. Nature 477, 549-555 (2011). | |
| Kruse, A. C., Hu, J., Pan, A. C., Arlow, D. H., Rosenbaum, D. M., Rosemond, E., Green, H. F., Liu, T., Chae, P. S., Dror, R. O., Shaw, D. E., Weis, W. I., Wess, J. & Kobilka, B. K. Structure and dynamics of the M3 muscarinic acetylcholine receptor. Nature 482, 552-556 (2012). | |
| Haga, K., Kruse, A. C., Asada, H., Yurugi-Kobayashi, T., Shiroishi, M., Zhang, C., Weis, W. I., Okada, T., Kobilka, B. K., Haga, T. & Kobayashi, T. Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonist. Nature 482, 547-551 (2012). | |
| Manglik, A., Kruse, A. C., Kobilka, T. S., Thian, F. S., Mathiesen, J. M., Sunahara, R. K., Pardo, L., Weis, W. I., Kobilka, B. K. & Granier, S. Crystal structure of the µ-opioid receptor bound to a morphinan antagonist. Nature 485, 321-326 (2012). | |
Granier, S., Manglik, A., Kruse, A. C., Kobilka, T. S., Thian, F. S., Weis, W. I., and Kobilka, B. K. Structure of the delta-opioid receptor bound to naltrindole, Nature 485, 400-404 (2012). |