Selected Publications

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Download 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.
Download PDF Download 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.
Download PDF Download Gether, U. and Kobilka, B.K. G Protein-coupled Receptors: Mechanism of Agonist activation. J. Biol. Chem. 1997. 273: p. 17979-82.
Download PDF Download 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.
Download PDF Download 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.
Download PDF Download 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.
Download PDF Download 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.
Download PDF Download 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.
Download PDF Download 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.
Download PDF Download 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.
Download PDF Download 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.
Download PDF Download 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.
Download PDF Download 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.
Download PDF Download 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.
Download PDF Download 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.
Download PDF Download 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.
Download PDF Download 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.
Download PDF Download 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.
Download PDF Download 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.
Download PDF Download 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.
Download PDF Download 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..
Download PDF Download 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.
Download PDF Download Y. Xiang and B. Kobilka, Myocyte Adrenoceptor Signaling Pathways. Science, 2003. 300: p 1530-1532.
Download PDF Download 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.
Download PDF Download 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.
Download PDF Download 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.
Download PDF Download Kobilka, B.K. Agonist binding: a multistep process.
Mol Pharmacol. 2004 May;65(5):1060-2.
Download PDF Download Parnot, C. and Kobilka, B.K. Toward understanding GPCR dimers. Nat Struct Mol Biol. 2004 Aug;11(8):691-2.
Download PDF Download 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.
Download PDF Download 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.
Download PDF Download 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.
Download PDF Download 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.
Download PDF Download 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.
Download PDF Download 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.
Download PDF Download Kobilka, B.K. and Deupi, X., Conformational complexity of G-protein-coupled receptors. Trends Pharmacol Sci, 2007. 28(8): p. 397-406.
Download PDF Download 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.
Download PDF Download Kobilka, B.K. and Deupi, X., Conformational complexity of G-protein-coupled receptors. Trends Pharmacol Sci, 2007.

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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.

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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.

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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.

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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.
Download PDF Download 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.
Download PDF Download 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.
Download PDF Download 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.
Download PDF Download Rosenbaum, D.M., Rasmussen, S.G., Kobilka, B.K. The structure and function of G-protein-coupled receptors. Nature, 2009. 459(7245): 356-363.

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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.

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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).

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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).

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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).

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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).

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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).

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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).

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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).

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Zhang, C., Srinivasan, Y., Arlow, D. H., Fung, J. J., Palmer, D., Zheng, Y., Green, H. F., Pandey, A., Dror, R. O., Shaw, D. E., Weis, W. I., Coughlin, S. R. & Kobilka, B. K. High-resolution crystal structure of human protease-activated receptor 1. Nature, 492, 387-392 (2012).

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Nygaard, R., Zou, Y., Dror, R. O., Mildorf, T. J., Arlow, D. H., Manglik, A., Pan, A. C., Liu, C. W., Fung, J. J., Bokoch, M. P., Thian, F. S., Kobilka, T. S., Shaw, D. E., Mueller, L., Prosser, R. S. & Kobilka, B. K. The Dynamic Process of beta(2)-Adrenergic Receptor Activation. Cell 152, 532-542 (2013).