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Robert J. Lefkowitz
Researcher at Howard Hughes Medical Institute
Publications - 867
Citations - 153371
Robert J. Lefkowitz is an academic researcher from Howard Hughes Medical Institute. The author has contributed to research in topics: Receptor & G protein-coupled receptor. The author has an hindex of 214, co-authored 860 publications receiving 147995 citations. Previous affiliations of Robert J. Lefkowitz include University of Nice Sophia Antipolis & University of Stuttgart.
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A quantitative analysis of beta-adrenergic receptor interactions: resolution of high and low affinity states of the receptor by computer modeling of ligand binding data
TL;DR: The properties of ligand binding to the beta-adrenergic receptor have been studied using a computer modeling technique to analyze data obtained by indirect binding methods and the ability of an agonist to activate adenylate cyclase correlates closely with the amount of high affinity state formed in the presence of the agonist.
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Molecular Mechanism of β-Arrestin-Biased Agonism at Seven-Transmembrane Receptors
TL;DR: One particular class of biased ligands has the ability to alter the balance between G protein-dependent and β-arrestin-dependent signal transduction and support the notion that biased agonists may identify new classes of therapeutic agents that have fewer side effects.
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Essential Role for G Protein-coupled Receptor Endocytosis in the Activation of Mitogen-activated Protein Kinase
Yehia Daaka,Louis M. Luttrell,Seungkirl Ahn,Gregory J. Della Rocca,Stephen S. G. Ferguson,Marc G. Caron,Robert J. Lefkowitz +6 more
TL;DR: These paradigms are inadequate to account for GPCR-mediated, Ras-dependent activation of the mitogen-activated protein (MAP) kinases Erk1 and -2, and β2-adrenergic receptor-mediated activation of MAP kinase is inhibited in HEK293 cells expressing dominant suppressor mutants of β-arrestin or dynamin.
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Beta-arrestin2, a novel member of the arrestin/beta-arrestin gene family.
Havard Attramadal,J. L. Arriza,Chiye Aoki,T. M. Dawson,J. Codina,Madan M. Kwatra,S. H. Snyder,Marc G. Caron,Robert J. Lefkowitz +8 more
TL;DR: Immunohistochemical analysis of the tissue distribution of beta-Arrestin1 and beta-arrestin2 in rat brain shows extensive, but heterogenous, neuronal labeling of the two proteins, suggesting that they have relatively broad receptor specificity regulating many G protein-coupled receptors.
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A unique mechanism of β-blocker action: Carvedilol stimulates β-arrestin signaling
James W. Wisler,Scott M. DeWire,Erin J. Whalen,Jonathan D. Violin,Matthew T. Drake,Seungkirl Ahn,Sudha K. Shenoy,Robert J. Lefkowitz +7 more
TL;DR: Data indicate that carvedilol is able to stabilize a receptor conformation which, although uncoupled from Gs, is nonetheless able to stimulate β-arrestin-mediated signaling, and it is hypothesized that such signaling may contribute to the special efficacy of carveilol in the treatment of heart failure.