Nguyen, A.H. and Lefkowitz, R.J. Signaling at the endosome: cryo-EM structure of a GPCR–G protein–beta-arrestin megacomplex. The FEBS Journal. Feb, 2021. In press.
Pakharukova, N., Masoudi, A., Pani, B., Staus, D.P., and Lefkowitz, R.J. Allosteric activation of proto-oncogene kinase Src by GPCR–beta-arrestin complexes. Journal of Biological Chemistry. Dec 4, 2020, 295(49):16773-16784. PMID: 32978252
McMahon, C., Staus, D.P., Wingler, L.M., Wang, J., Skiba, M.A., Elgeti, M., Hubbell, W., Rockman, H.A., Kruse, A.C., and Lefkowitz, R.J. Synthetic nanobodies as angiotensin receptor blockers. PNAS. Aug 18, 2020,117(33):20284-20291. PMCID: PMC7443875
Wingler, L.M. and Lefkowitz, R.J. Conformational basis of G protein-coupled receptor signaling versatility. Trends Cell Biol. Sep 2020, 30(9):736-747. PMCID: PMC7483927
Manglik, A., Wingler, L.M., Rockman, H.A., and Lefkowitz, R.J. β-Arrestin-Biased Angiotensin II Receptor Agonists for COVID-19. Circulation. Jul 28, 2020,142(4):318-320. PMCID: PMC7382535
Kim, J., Grotegut, C.A., Wisler, J.W., Mao, L., Rosenberg, P.B., Rockman, H.A., and Lefkowitz, R.J. The β-arrestin biased β-adrenergic receptor blocker carvedilol enhances skeletal muscle contractility. PNAS. June 2, 117 (22): 12435-12443, 2020. PMCID: PMC6309084
Staus, D.P., Hu, H., Robertson, M.J., Kleinhenz, A.L.W., Wingler, L.M., Capel, W.D., Latorraca, N.R., Lefkowitz, R.J, and Skiniotis, G. Structure of the M2 Muscarinic Receptor-β-arrestin Complex in a Lipid Nanodisc. Nature. Mar; 579(7798):297-302, 2020. PMCID: PMC7367492
Wingler, L.M., Skiba, M.A., McMahon, C., Staus, D.P., Kleinhenz, A.L.W., Suomivuori, C-M, Latorraca, N.R., Dror, R.O., Lefkowitz, R.J., and Kruse, A.C. Angiotensin and Biased Analogs Induce Structurally Distinct Active Conformations within a GPCR. Science. Feb 21, Vol. 367, Issue 6480, pp. 888-892, 2020.
Suomivuori, C-M, Latorraca, N.R., Wingler, L.M., Eismann, S., King, M.C., Klenhenz, A.L.W., Skiba, M.A., Staus, D.P., Kruse, A.C., Lefkowitz, R.J., and Dror, R.O. Molecular Mechanism of Biased Signaling in a Prototypical G-Protein-Coupled Receptor. Science. Feb 21, Vol. 367, Issue 6480, pp. 881-887, 2020.
Staus, D.P., Hu, H., Robertson, M.J., Kleinhenz, A.L.W., Wingler, L.M., Capel, W.D., Latorraca, N.R., Lefkowitz, R.J, and Skiniotis, G. Structure of the M2 Muscarinic Receptor-β-arrestin Complex in a Lipid Nanodisc.Nature. Jan 16, 2020. doi: 10.1038/s41586-020-1954-0. Epub link:
Jain, M.K., Yamada, T., Lefkowitz, R.J. We Need More Doctors Who Are Scientists. New York Times. Sept. 23, 2019.
Nguyen, A.H., Thomsen, A.R.B., Cahill III, T.J., Huang, R., Huang, L., Marcink, T., Clarke, O.B., Hissel, S., Masoudi, A., Ben-Hail, D., Samaan, F., Dandey, V.P., Tan, Y.Z., Hong, C., Mahoney, J.P., Triest, S., Little IV, J., Chen, X., Sunahara, R., Steyaert, J., Molina, H., Yu, Z., des Georges, A., Lefkowitz, R.J. Structure of an Endosomal Signaling GPCR-G Protein-β-arrestin Mega-Complex.Nature Structural and Molecular Biology. Dec; 26(12):1123-1131, 2019.
Jain, M.K., Cheung, V.G., Utz, P.J., Kobilka, B.K., Yamada, T., Lefkowitz, R.J. Saving the Endangered Physican-Scientist – A Plan for Accelerating Medical Breakthroughs. N Engl J Med. August 1; 381:399-402, 2019.
Staus, D.P., Wingler, L.M., Pichugin, D., Prosser, R.S., Lefkowitz, R.J. Detergent- and Phospholipid-Based Reconstitution Systems Have Differential Effects on Constitutive Activity of G-Protein-Coupled Receptors. J. Biol, Chem. July 30; 294(36):13218-13223, 2019.
Liu, X., Masoudi, A., Kahsai, A.W., Huang, L.Y., Pani, B., Staus, D.P., Shim, P.J., Hirata, K., Simhal, R.K., Schwalb, A.M., Rambarat, P.K., Ahn, S., Lefkowitz, R.J., Kobilka, B. Mechanism of β2AR Regulation by an Intracellular Positive Allosteric Modulator. Science. June 28; 364(6447): 1283-1287, 2019.
Wingler, L.M., McMahon, C., Staus, D.P., Lefkowitz, R.J., Kruse, A.C. Distinctive Activation Mechanism for Angiotensin Receptor Revealed by a Synthetic Nanobody. Cell. Jan. 24; 176(3): 479-490, 2019.
Wingler, L.M., Elgeti, M., Hilger, D., Latorraca, N.R., Lerch, M.T., Staus, D.P., Dror, R.O., Kobilka, B.K., Hubbell, W.L., Lefkowitz, R.J. Angiotensin Analogs with Divergent Bias Stabilize Distinct Receptor Conformations. Cell. Jan. 24; 176(3): 468-478, 2019. PMCID: PMC6475118.
Kim, J., Grotegut, C.A., Wisler, J.W., Li, T., Mao, L., Chen, M, Chen, W., Rosenberg, P.B, Rockman, H.A., Lefkowitz, R.J. β-arrestin 1 regulates β2-adrenergic receptor-mediated skeletal muscle hypertrophy and contractility. Skeletal Muscle. Dec. 27; 8(1):39, 2018. PMCID: PMC6309084.
Luttrell, L.M., Wang, J., Plouffe, B., Smith, J.S., Yamani, L., Kaur, S., Jean-Charles, P.Y., Gauthier, C., Lee, M.H., Pani, B., Kim, J., Ahn, S., Rajagopal, S., Reiter, E., Bouvier, M., Shenoy, S.K., Laporte, S.A., Rockman, H.A., Lefkowitz, R.J. Manifold roles of β-arrestins in GPCR signaling elucidated with siRNA and CRISPR/Cas9. Science Signaling.Sept. 25; 11(549), 2018. PMCID: PMC6369040.
Kahsai, A.W., Pani, B., Lefkowitz, R.J. GPCR Signaling: Conformational Activation of Arrestins.Cell Research. Aug; 28(8):783-784, 2018. PMCID: PMC6082894.
Wisler, J.W., Rockman, H.A., Lefkowitz, R.J. Biased G-Protein-Coupled Receptor Signaling: Changing the Paradigm of Drug Discovery. Circulation. May 29; 137(22): 2315-2317, 2018. PMCID: PMC5984047.
Choi, M., Staus, D.P., Wingler, L.M., Ahn, S., Pani, B., Capel, W.D., Lefkowitz, R.J. G Protein-Coupled Receptor Kinases (GRKs) Orchestrate Biased Agonism at the β2-adrenergic Receptor. Science Signaling. Aug.21; 11(544), 2018. PMID: 30131371.
Ahn, S., Pani, B., Kahsai, A.W., Olsen, E.K., Husemoen, G., Vestrgaard, M., Jin, L., Zhao, S., Wingler, L.M., Rambarat, P.K., Simhal, R.K., Xu, T.T. Sun, L.D., Shim, P.J., Strachan, R.T., Staus, D.P., Huang, L-Y., Franch, T., Chen, X, Lefkowitz, R.J. Small Molecule Positive Allosteric Modulators of the β2-Adrenoceptor Isolated from DNA Encoded Libraries. Molecular Pharmacology. Aug; 94(2):850-861, 2018. PMCID: PMC6022804.
Staus, D.P., Wingler, L.M., Choi, M., Pani, B., Manglik, A., Kruse, A.C., Lefkowitz, R.J. Sortase Ligation Enables Homogeneous GPCR Phosphorylation to Reveal Diversity in β-arrestin Coupling. PNAS. Apr.10; 115(15): 3834-3839, 2018. PMCID: PMC5899476.
Smith JS, Lefkowitz RJ, Ragaopal S. Biased signaling: from simple switches to allosteric microprocessors. Nat Rev Drug Discov. Apr;17(4):243-260, 2018.
Lefkowitz, R.J., A Serendipitous Scientist, Annu Rev Pharmacol Toxicol. Jan 6;58:17-32, 2018.
Rein, L.A.M., Wisler, J.W., Kim, J., Theriot, B., Huang, L., Price, T., Yang, H., Chen, M., Chen, W., Sipkins, D., Fedoriw, Y., Walker, J.K.L., Premont, R.T., Lefkowitz, R.J. β-arrestin2 mediates progression of murine primary myelofibrosis. JCI insight. Dec 21; 2(24), 2017. PMCID: PMC5752278.
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