Author details

Full Name

Robert J Lefkowitz

Affiliation

ORCID

Career Start Year

1956

Papers

812

H Index

209

Expertise

CM4AI Collaborator

PMID	Paper Title	Journal Title	Published Year
37432742	Allosteric modulator potentiates Î²2AR agonist-promoted bronchoprotection in asthma models.		2023
36961836	Loss of biased signaling at a G protein-coupled receptor in overexpressed systems.		2023
35171650	Translating science to medicine: The case for physician-scientists.	Sci Transl Med	2022
35483373	GPCR-mediated Î²-arrestin activation deconvoluted with single-molecule precision.	Cell	2022
35915165	Marc G. Caron (1946-2022).	Nature Neuroscience	2022
34757127	The GPCR-Î²-arrestin complex allosterically activates C-Raf by binding its amino terminus.	Journal of Biological Chemistry	2021
33605032	Signaling at the endosome: cryo-EM structure of a GPCR-G protein-beta-arrestin megacomplex.		2021
34580163	Unique Positive Cooperativity Between the -Arrestin-Biased -Blocker Carvedilol and a Small Molecule Positive Allosteric Modulator of the 2-Adrenergic Receptor.	Molecular Pharmacology	2021
34561298	-Arrestin-Biased Allosteric Modulator Potentiates Carvedilol-Stimulated Adrenergic Receptor Cardioprotection.	Molecular Pharmacology	2021
32888497	SnapShot: Î²-Arrestin Functions.	Cell	2020
32079768	Angiotensin and biased analogs induce structurally distinct active conformations within a GPCR.	Science	2020
32079767	Molecular mechanism of biased signaling in a prototypical G protein-coupled receptor.	Science	2020
32414934	The Î²-arrestin-biased Î²-adrenergic receptor blocker carvedilol enhances skeletal muscle contractility.	Proceedings of the National Academy of Sciences of the United States of America	2020
32412788	Î²-Arrestin-Biased Angiotensin II Receptor Agonists for COVID-19.	Circulation	2020
31945772	Structure of the M2 muscarinic receptor-Î²-arrestin complex in a lipid nanodisc.	Nature	2020
32978252	Allosteric activation of proto-oncogene kinase Src by GPCR-beta-arrestin complexes.	Journal of Biological Chemistry	2020
32753386	Synthetic nanobodies as angiotensin receptor blockers.	Proc Natl Acad Sci U S A	2020
32622699	Conformational Basis of G Protein-Coupled Receptor Signaling Versatility.	Trends in Cell Biology	2020
31362983	Detergent- and phospholipid-based reconstitution systems have differential effects on constitutive activity of G-protein-coupled receptors.	Journal of Biological Chemistry	2019
31740855	Structure of an endosomal signaling GPCR-G protein-Î²-arrestin megacomplex.	Nat Struct Mol Biol	2019
30639100	Distinctive Activation Mechanism for Angiotensin Receptor Revealed by a Synthetic Nanobody.	Cell	2019
30639099	Angiotensin Analogs with Divergent Bias Stabilize Distinct Receptor Conformations.	Cell	2019
31365796	Saving the Endangered Physician-Scientist - A Plan for Accelerating Medical Breakthroughs.	New England Journal of Medicine	2019
29769246	Small-Molecule Positive Allosteric Modulators of the -Adrenoceptor Isolated from DNA-Encoded Libraries.	Molecular Pharmacology	2018
28715979	A Serendipitous Scientist.	Annual Review of Pharmacology and Toxicology	2018
30030517	GPCR signaling: conformational activation of arrestins.	Cell Research	2018
30591079	Î²-arrestin 1 regulates Î²2-adrenergic receptor-mediated skeletal muscle hypertrophy and contractility.	Skeletal Muscle	2018
30254056	Manifold roles of Î²-arrestins in GPCR signaling elucidated with siRNA and CRISPR/Cas9.	Sci Signal	2018
30131371	G protein-coupled receptor kinases (GRKs) orchestrate biased agonism at the Î²-adrenergic receptor.	Science Signaling	2018
29302067	Biased signalling: from simple switches to allosteric microprocessors.	Nature Reviews Drug Discovery	2018
29581292	Sortase ligation enables homogeneous GPCR phosphorylation to reveal diversity in Î²-arrestin coupling.	Proc Natl Acad Sci U S A	2018
29844068	Biased G Protein-Coupled Receptor Signaling: Changing the Paradigm of Drug Discovery.	Circulation	2018
28130548	Allosteric "beta-blocker" isolated from a DNA-encoded small molecule library.	Proceedings of the National Academy of Sciences of the United States of America	2017
28813418	Mechanism of intracellular allosteric Î²AR antagonist revealed by X-ray crystal structure.	Nature	2017
28329674	Î²-Arrestin2 Couples Metabotropic Glutamate Receptor 5 to Neuronal Protein Synthesis and Is a Potential Target to Treat Fragile X.	Cell Rep	2017
29263312	Î²-Arrestin2 mediates progression of murine primary myelofibrosis.	JCI insight	2017
28223524	Distinct conformations of GPCR-Î²-arrestin complexes mediate desensitization, signaling, and endocytosis.	Proc Natl Acad Sci U S A	2017
27499021	GPCR-G Protein-Î²-Arrestin Super-Complex Mediates Sustained G Protein Signaling.	Cell	2016
26791713	Alfred Goodman Gilman (1941-2015).	Nature	2016
27409812	Allosteric nanobodies reveal the dynamic range and diverse mechanisms of G-protein-coupled receptor activation.	Nature	2016
27398998	Conformationally selective RNA aptamers allosterically modulate the Î²2-adrenoceptor.	Nature Chemical Biology	2016
26237039	Inspiring the next generation of physician-scientists.	Journal of Clinical Investigation	2015
26371162	The role of Î²-arrestin2-dependent signaling in thoracic aortic aneurysm formation in a murine model of Marfan syndrome.	Am J Physiol Heart Circ Physiol	2015
25170081	Allosteric modulation of Î²-arrestin-biased angiotensin II type 1 receptor signaling by membrane stretch.	Journal of Biological Chemistry	2014
24319111	Regulation of Î²2-adrenergic receptor function by conformationally selective single-domain intrabodies.	Molecular Pharmacology	2014
25043026	Visualization of arrestin recruitment by a G-protein-coupled receptor.	Nature	2014
24680426	Recent developments in biased agonism.	Current Opinion in Cell Biology	2014
24668815	Divergent transducer-specific molecular efficacies generate biased agonism at a G protein-coupled receptor (GPCR).	Journal of Biological Chemistry	2014
23650015	A brief history of G-protein coupled receptors (Nobel Lecture).	Angewandte Chemie - International Edition	2013
24454993	Discovery of Î²2 Adrenergic Receptor Ligands Using Biosensor Fragment Screening of Tagged Wild-Type Receptor.	ACS Med Chem Lett	2013