Faculty Profiles

Robert J. Lefkowitz
Professor of Chemistry
Office: 
467 Clin & Res Labs, Durham, NC 27710
Phone: 
(919) 684-2974
Fax: 
(919) 684-8875

Overview

Education:

Resident, Medicine, Massachusetts General Hospital 1970 - 1971

Resident, Medicine, Columbia University 1967 - 1968

Intern, Medicine, Columbia University 1966 - 1967

M.D., Columbia University 1966

Choi, M, Staus, DP, Wingler, LM, Ahn, S, Pani, B, Capel, WD, and Lefkowitz, RJ. "G protein-coupled receptor kinases (GRKs) orchestrate biased agonism at the β2-adrenergic receptor." Science Signaling 11.544 (August 21, 2018). Full Text

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

Lefkowitz, RJ. "A Serendipitous Scientist." Annual review of pharmacology and toxicology 58 (January 2018): 17-32. 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

Pages

Bond, RA, and Lefkowitz, RJ. Historical Background and Introduction. April 25, 2006. 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.

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.

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.

Pages

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--.