Faculty Profiles

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



Resident, Medicine, Massachusetts General Hospital 1970 - 1971

Resident, Medicine, Columbia University 1967 - 1968

Intern, Medicine, Columbia University 1966 - 1967

M.D., Columbia University 1966

Wingler, Laura M., et al. “Angiotensin Analogs with Divergent Bias Stabilize Distinct Receptor Conformations..” Cell, vol. 176, no. 3, Jan. 2019, pp. 468-478.e11. Pubmed, doi:10.1016/j.cell.2018.12.005. Full Text

Wingler, Laura M., et al. “Distinctive Activation Mechanism for Angiotensin Receptor Revealed by a Synthetic Nanobody..” Cell, vol. 176, no. 3, Jan. 2019, pp. 479-490.e12. Pubmed, doi:10.1016/j.cell.2018.12.006. Full Text

Kim, Jihee, et al. “β-arrestin 1 regulates β2-adrenergic receptor-mediated skeletal muscle hypertrophy and contractility..” Skelet Muscle, vol. 8, no. 1, Dec. 2018. Pubmed, doi:10.1186/s13395-018-0184-8. Full Text

Luttrell, Louis M., et al. “Manifold roles of β-arrestins in GPCR signaling elucidated with siRNA and CRISPR/Cas9..” Sci Signal, vol. 11, no. 549, Sept. 2018. Pubmed, doi:10.1126/scisignal.aat7650. Full Text

Choi, Minjung, et al. “G protein-coupled receptor kinases (GRKs) orchestrate biased agonism at the β2-adrenergic receptor..” Sci Signal, vol. 11, no. 544, Aug. 2018. Pubmed, doi:10.1126/scisignal.aar7084. Full Text

Ahn, Seungkirl, et al. “Small-Molecule Positive Allosteric Modulators of the β2-Adrenoceptor Isolated from DNA-Encoded Libraries..” Mol Pharmacol, vol. 94, no. 2, Aug. 2018, pp. 850–61. Pubmed, doi:10.1124/mol.118.111948. Full Text

Kahsai, Alem W., et al. “GPCR signaling: conformational activation of arrestins..” Cell Res, vol. 28, no. 8, Aug. 2018, pp. 783–84. Pubmed, doi:10.1038/s41422-018-0067-x. Full Text

Wisler, James W., et al. “Biased G Protein-Coupled Receptor Signaling: Changing the Paradigm of Drug Discovery..” Circulation, vol. 137, no. 22, May 2018, pp. 2315–17. Pubmed, doi:10.1161/CIRCULATIONAHA.117.028194. Full Text

Staus, Dean P., et al. “Sortase ligation enables homogeneous GPCR phosphorylation to reveal diversity in β-arrestin coupling..” Proc Natl Acad Sci U S A, vol. 115, no. 15, Apr. 2018, pp. 3834–39. Pubmed, doi:10.1073/pnas.1722336115. Full Text

Smith, Jeffrey S., et al. “Biased signalling: from simple switches to allosteric microprocessors..” Nat Rev Drug Discov, vol. 17, no. 4, Apr. 2018, pp. 243–60. Pubmed, doi:10.1038/nrd.2017.229. Full Text


Bond, R. A., and R. J. Lefkowitz. Historical Background and Introduction. Vol. 24, 2006, pp. 1–10. Scopus, doi:10.1002/352760734X.ch1. Full Text

Lefkowitz, R. J., et al. Biochemical mechanisms for regulation of β adrenergic receptors by β adrenergic agonists. Vol. No. 402, 1977, pp. 502–06.

Rein, Lindsay A. M., et al. “beta-arrestin2 Is Necessary for Development of MPLW515L Mutant Primary Myelofibrosis.” Blood, vol. 126, no. 23, AMER SOC HEMATOLOGY, 2015.

Shukla, Arun K., et al. “Crystal structure of active Beta-arrestin1 bound to phosphorylated carboxy-terminus of a G protein-coupled receptor.” Faseb Journal, vol. 27, FEDERATION AMER SOC EXP BIOL, 2013.

Patel, Chetan B., et al. “A Modified beta 1-adrenergic Receptor Demonstrates Bias Towards G Protein Receptor Kinase Phosphorylation.” Circulation, vol. 120, no. 18, LIPPINCOTT WILLIAMS & WILKINS, 2009, pp. S800–01.

Wang, Jiangbo, et al. “Targeting hedgehog signaling in medulloblastoma.” Neuro Oncology, vol. 9, no. 4, DUKE UNIV PRESS, 2007, pp. 560–61.

Lefkowitz, R. J. “Seven transmembrane receptors: something old, something new.” Acta Physiologica, vol. 190, no. 1, WILEY, 2007, pp. 9–19. Wos, doi:10.1111/j.1748-1716.2007.01693.x. Full Text

Chen, Juhsien, et al. “beta-arrestin mediated beta 1-adrenergic receptor transactivartion of the epidermal growth factor receptor requires GRK 5 and 6.” Circulation, vol. 114, no. 18, LIPPINCOTT WILLIAMS & WILKINS, 2006, pp. 159–159.

Kim, Jihee, et al. “beta-arrestins regulate proliferation and migration of smooth muscle cells in vitro & in vivo: Isoform-specific roles.” Circulation, vol. 114, no. 18, LIPPINCOTT WILLIAMS & WILKINS, 2006, pp. 296–296.

Shenoy, Sudha K., and Robert J. Lefkowitz. “Beta-arrestin-dependent signaling by seven-transmembrane receptors.” Regulatory Peptides, vol. 135, no. 3, ELSEVIER SCIENCE BV, 2006, pp. 102–102.

Nobles, K. N., et al. “Conformational changes in beta-arrestin1: The importance of beta-arrestin1's N-domain.” Faseb Journal, vol. 20, no. 4, FEDERATION AMER SOC EXP BIOL, 2006, pp. A114–A114.


Willerson, J. T. “Cardiac function in mice overexpressing the beta-adrenergic receptor kinase or a beta ARK inhibitor..” Circulation, vol. 92, no. 3, 1 Aug. 1995.