Resident, Medicine, Massachusetts General Hospital 1970 - 1971
Resident, Medicine, Columbia University 1967 - 1968
Intern, Medicine, Columbia University 1966 - 1967
M.D., Columbia University 1966
Ahn, S, Pani, B, Kahsai, AW, Olsen, EK, Husemoen, G, Vestergaard, M, Jin, L, Zhao, S, Wingler, LM, Rambarat, PK, Simhal, RK, Xu, TT, Sun, LD, Shim, PJ, Staus, DP, Huang, L-Y, Franch, T, Chen, X, and Lefkowitz, RJ. "Small-Molecule Positive Allosteric Modulators of the β2-Adrenoceptor Isolated from DNA-Encoded Libraries." Molecular Pharmacology 94.2 (August 2018): 850-861. Full Text
Kahsai, AW, Pani, B, and Lefkowitz, RJ. "GPCR signaling: conformational activation of arrestins." Cell Research 28.8 (August 2018): 783-784. Full Text
Wisler, JW, Rockman, HA, and Lefkowitz, RJ. "Biased G Protein-Coupled Receptor Signaling: Changing the Paradigm of Drug Discovery." Circulation 137.22 (May 2018): 2315-2317. Full Text
Smith, JS, Lefkowitz, RJ, and Rajagopal, S. "Biased signalling: from simple switches to allosteric microprocessors." Nature Reviews. Drug Discovery 17.4 (April 2018): 243-260. (Review) Full Text
Staus, DP, Wingler, LM, Choi, M, Pani, B, Manglik, A, Kruse, AC, and Lefkowitz, RJ. "Sortase ligation enables homogeneous GPCR phosphorylation to reveal diversity in β-arrestin coupling." Proceedings of the National Academy of Sciences of the United States of America 115.15 (April 2018): 3834-3839. Full Text
Liu, X, Ahn, S, Kahsai, AW, Meng, K-C, Latorraca, NR, Pani, B, Venkatakrishnan, AJ, Masoudi, A, Weis, WI, Dror, RO, Chen, X, Lefkowitz, RJ, and Kobilka, BK. "Mechanism of intracellular allosteric β2AR antagonist revealed by X-ray crystal structure." Nature 548.7668 (August 16, 2017): 480-484. Full Text
Cahill, TJ, Thomsen, ARB, Tarrasch, JT, Plouffe, B, Nguyen, AH, Yang, F, Huang, L-Y, Kahsai, AW, Bassoni, DL, Gavino, BJ, Lamerdin, JE, Triest, S, Shukla, AK, Berger, B, Little, J, Antar, A, Blanc, A, Qu, C-X, Chen, X, Kawakami, K, Inoue, A, Aoki, J, Steyaert, J, Sun, J-P, Bouvier, M, Skiniotis, G, and Lefkowitz, RJ. "Distinct conformations of GPCR-β-arrestin complexes mediate desensitization, signaling, and endocytosis." Proceedings of the National Academy of Sciences of the United States of America 114.10 (March 2017): 2562-2567. Full Text
Stoppel, LJ, Auerbach, BD, Senter, RK, Preza, AR, Lefkowitz, RJ, and Bear, MF. "β-Arrestin2 Couples Metabotropic Glutamate Receptor 5 to Neuronal Protein Synthesis and Is a Potential Target to Treat Fragile X." Cell reports 18.12 (March 2017): 2807-2814. Full Text
Ahn, S, Kahsai, AW, Pani, B, Wang, Q-T, Zhao, S, Wall, AL, Strachan, RT, Staus, DP, Wingler, LM, Sun, LD, Sinnaeve, J, Choi, M, Cho, T, Xu, TT, Hansen, GM, Burnett, MB, Lamerdin, JE, Bassoni, DL, Gavino, BJ, Husemoen, G, Olsen, EK, Franch, T, Costanzi, S, Chen, X, and Lefkowitz, RJ. "Allosteric "beta-blocker" isolated from a DNA-encoded small molecule library." Proceedings of the National Academy of Sciences of the United States of America 114.7 (February 2017): 1708-1713. Full Text
Lefkowitz, RJ, Mukherjee, C, and Caron, M. Biochemical mechanisms for regulation of β adrenergic receptors by β adrenergic agonists. January 1, 1977.
Rein, LAM, Wisler, JW, Theriot, BS, Huang, L-Y, Premont, RT, and Lefkowitz, RJ. "beta-arrestin2 Is Necessary for Development of MPLW515L Mutant Primary Myelofibrosis." December 3, 2015.
Shukla, AK, Manglik, A, Kruse, A, Reis, R, Tseng, WC, Staus, DP, Hilger, D, Uysal, S, Huang, L, Peduch, M, Tripathi-Shukla, P, Koide, A, Koide, S, Weis, WI, Kossiakoff, AK, Kobilka, BK, and Lefkowitz, RJ. "Crystal structure of active Beta-arrestin1 bound to phosphorylated carboxy-terminus of a G protein-coupled receptor." April 2013.
Maudsley, S, Liao, S, Yuan, L, Lefkowitz, RJ, Luttrell, LM, and Gesty-Palmer, D. "The Unique Efficacy Profile of a beta-Arrestin Pathway-Selective Parathyroid Hormone Receptor Agonist Revealed by Metabolic Pathways Analysis." June 2010.
Patel, CB, Patel, PA, Frangakis, SG, Chen, M, Shenoy, SK, Lefkowitz, RJ, and Rockman, HA. "A Modified beta 1-adrenergic Receptor Demonstrates Bias Towards G Protein Receptor Kinase Phosphorylation." November 3, 2009.
Wang, J, Liu, R, Bond, M, Chen, M, Singh, S, Ali-Osman, F, Lefkowitz, RJ, Diehl, AM, Lyerly, HK, Barak, L, and Chen, W. "Targeting hedgehog signaling in medulloblastoma." October 2007.
Lefkowitz, RJ. "Seven transmembrane receptors: something old, something new." May 2007. Full Text
Chen, J, Naga Prasad, SV, Tilley, DG, Lefkowitz, RJ, and Rockman, HA. "beta-arrestin mediated beta 1-adrenergic receptor transactivartion of the epidermal growth factor receptor requires GRK 5 and 6." October 31, 2006.
Kim, J, Zhang, L, Peppel, K, Lefkowitz, RJ, and Freedman, NJ. "beta-arrestins regulate proliferation and migration of smooth muscle cells in vitro & in vivo: Isoform-specific roles." October 31, 2006.
Shenoy, SK, and Lefkowitz, RJ. "Beta-arrestin-dependent signaling by seven-transmembrane receptors." August 30, 2006.
Nobles, KN, Guan, ZQ, Xiao, KH, Oas, TG, and Lefkowitz, RJ. "Conformational changes in beta-arrestin1: The importance of beta-arrestin1's N-domain." March 6, 2006.
Koch, WJ, Rockman, HA, Samama, P, Hamilton, RA, Bond, RA, Milano, CA, and Lefkowitz, RJ. "Cardiac function in mice overexpressing the β-adrenergic receptor kinase or a βARK inhibitor." Circulation 92.3 (1995): 277--.