Robert J. Lefkowitz MD

Nobel Prize in Chemistry 2012
National Medal of Science- Biological Sciences 2007 USA

Physician- Cardiologist, Scientist. G-protein-coupled receptors;
approximately half of all medicines used today use this kind of receptor.

"Strong family history of coronary artery disease ... at age 50 I had quadruple bypass surgery [1994]. I minimize my risk factors with daily physical exercise, a vegetarian diet and appropriate medications".

Patents


Publication:	1/10
Publication No:	US 10682397 B2
Title:	Methods of treating fragile X syndrome and related disorders
Publication Type:	United States Utility Patent
Publication Date:	June 16, 2020
Filing Date:	Nov. 30, 2016
Inventors:	Benjamin David Auerbach, Mark Firman Bear, Laura Jane Stoppel, Robert J. Lefkowitz
Assignee:	Massachusetts Institute Of Technology, Duke University
Abstract:	Disclosed herein are novel methodologies of treating fragile X syndrome and related disorders by inhibiting mGlu5-relevant signaling pathways via the reduction of β-arrestin2 protein levels or the diminution of mGlu5 and β-arrestin2 protein interactions.
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Publication:	2/10
Publication No:	US 7413876 B2
Title:	Expression of G protein coupled receptors in yeast
Publication Type:	United States Utility Patent
Publication Date:	Aug. 19, 2008
Filing Date:	Nov. 23, 2004
Inventors:	Klim King, Henrick G. Dohlman, Marc G. Caron, Robert J. Lefkowitz
Assignee:	Duke University Medical Center
Abstract:	Disclosed is a transformed yeast cell containing a first heterologous DNA sequence which codes for a mammalian G protein-coupled receptor and a second heterologous DNA sequence which codes for a mammalian G protein a subunit (mammalian Gα). The first and second heterologous DNA sequences are capable of expression in the cell, but the cell is incapable of expressing an endogenous G protein a-subunit (yeast Gα). The cells are useful for screening compounds which affect the rate of dissociation of Gα from Gβγ in a cell. Also disclosed is a novel DNA expression vector useful for making cells as described above. The vector contains a first segment comprising at least a fragment of the extreme amino-terminal coding sequence of a yeast G protein-coupled receptor. A second segment is positioned downstream from the first segment (and in correct reading frame therewith), with the second segment comprising a DNA sequence encoding a heterologous G protein-coupled receptor.
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Publication:	3/10
Publication No:	US 7615610 B2
Title:	Methods of treating fragile X syndrome and related disorders
Publication Type:	United States Utility Patent
Publication Date:	Nov. 10, 2009
Filing Date:	Jan. 26, 2004
Inventors:	Sudha Shenoy, Robert J. Lefkowitz
Assignee:	Duke University
Abstract:	The present invention relates to a modified arrestin which includes an arrestin molecule and a ubiquitin molecule. This modified arrestin has an increased affinity for a GPCR, and traffics with the GPCR into endosomes. The present invention further relates to a method of screening compounds and sample solutions for a GPCR agonist, antagonist, inverse agonist, or desensitization active compound. The modified arrestin is useful in the methods of the present invention.
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Publication:	4/10
Publication No:	AU 2003287006 B2
Title:	Expression of G protein coupled receptors in yeast
Publication Type:	Australian Patent
Publication Date:	March 18, 2010
Filing Date:	Oct 20, 2003
Inventors:	Walter J. Koch, Robert J. Lefkowitz, Claude A. Piantadosi, Jonathan S. Stamler, Erin J. Whalen
Assignee:	Duke University
Abstract:	Desensitization of receptors that control disease is prevented by inhibiting G-protein receptor kinases. This has applicability, e.g., for patients with heart failure or on a left ventricular heart device or a heart pump after surgery or about to undergo surgery and at high risk for a cardiac event of on an opiate or addicted to opiate or with cystic fibrosis or rheumatoid arthritis.
Representative Figure:	No Figure
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Publication:	5/10
Publication No:	US 7060871 B2
Title:	Use of exogenous β-adrenergic receptor and β-adrenergic receptor kinase gene constructs to enhance myocardial function
Publication Type:	United States Utility Patent
Publication Date:	June 13, 2006
Filing Date:	June 28, 2002
Inventors:	Walter J. Koch, Robert J. Lefkowitz, Carmelo A. Milano, Howard A. Rockman
Assignee:	Duke University
Abstract:	The present invention deals with gene therapy for treating chronic heart failure and other cardiac disease states which are accompanied by a reduced number or functioning of myocardial beta-adrenergic receptors (β-AR). β-AR receptor function is augmented in transgenic animals by delivery and expression of a beta-2-adrenergic receptor gene or a gene encoding a beta adrenergic receptor kinase inhibitor, resulting in increased in vivo left ventricular function. The present invention includes recombinant plasmid vectors, alternative beta-adrenergic receptor gene delivery strategies, and transgenic mice carrying a β-AR transgene, a β-ARK transgene, or a β-ARK inhibitor transgene.
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Publication:	6/10
Publication No:	US 6605424 B1
Title:	Method of detecting inhibitors of agonist-specific desensitization
Publication Type:	United States Utility Patent
Publication Date:	Aug. 12, 2003
Filing Date:	May 1, 2000
Inventors:	Robert J. Lefkowitz, Martin J. Lohse, Jeffrey L. Benovic, Marc G. Caron
Assignee:	Duke University
Abstract:	The present invention relates to a method of inhibiting desensitization of a cell to the effects of a compound. The method comprises contacting the cell with an agent capable of inhibiting phosphorylation, by a protein kinase, of a receptor for the compound present on the surface of the cell. The present invention also relates to a method of screening a compound for its ability to inhibit desensitization. The method comprises: i) contacting a receptor specific kinase-containing sample with the compound under conditions such that interaction between receptor specific kinase present in the sample and the compound can occur, and ii) determining the ability of the receptor specific kinase to phosphorylate the receptor for which it is specific.
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Publication:	7/10
Publication No:	US 6528271 B1
Title:	Inhibition of βarrestin mediated effects prolongs and potentiates opioid receptor-mediated analgesia
Publication Type:	United States Utility Patent
Publication Date:	March 4, 2003
Filing Date:	Dec.22, 1999
Inventors:	Laura M. Bohn, Fang-Tsyr Lin, Marc G. Caron, Robert J. Lefkowitz
Assignee:	Duke University
Abstract:	The present invention provides a βarrestin knockout mouse useful for screeening compounds for efficacy in controlling pain, methods of controlling pain in subjects by inhibiting binding of %beta;arrestin to phosphorylated μ opioid receptors, and methods of screening a compound for activity in potentiating μ opioid receptor agonist activity (e.g., morphine activity) by determining whether or not said compound inhibits βarrestin binding to a phosphorylated μ opioid receptor..
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Publication:	8/10
Publication No:	US 6683057 B1
Title:	Method of inhibiting smooth muscle cell proliferation
Publication Type:	United States Utility Patent
Publication Date:	March 4, 2003
Filing Date:	Dec. 22, 1999
Inventors:	Walter J. Koch, Robert J. Lefkowitz, Per-Otto Hagen
Assignee:	Duke University
Abstract:	he present invention relates, in general, to vascular smooth muscle proliferation and, in particular, to a method of inhibiting arterial and venous smooth muscle proliferation resulting, for example, from arterial injury or vein grafting. The invention also relates to an expression construct encoding a Gβγ inhibitor suitable for use in such a method.
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Publication:	9/10
Publication No:	US 6610532 B2
Title:	Intracellular inhibitors of Gq protein signaling
Publication Type:	United States Utility Patent
Publication Date:	Aug. 26, 2003
Filing Date:	July 24, 1998
Inventors:	Walter J. Koch, Robert J. Lefkowitz, Shahab A. Akhter, Louis M. Luttrell, Howard Rockman
Assignee:	Duke University
Abstract:	The present invention relates, in general, to myocardial hypertrophy and, in particular, to agents that inhibit cardiac Gq-coupled receptor signaling and to methods of inhibiting myocardial hypertrophy using same.
Representative Figure:	No Figure
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Publication:	10/10
Publication No:	US 5573908 A
Title:	Adrenergic receptor as a proto-oncogene
Publication Type:	United States Utility Patent
Publication Date:	Nov. 12, 1996
Filing Date:	Dec. 20, 1993
Inventors:	Lee F. Allen, Robert J. Lefkowitz, Marc G. Caron, Susanna Cotecchia
Assignee:	Duke Univesity
Abstract:	A recombinant cell comprising a host cell containing a recombinant DNA sequence is disclosed. The recombinant DNA sequence comprises vector DNA and DNA which encodes a mammalian adrenergic receptor. The host cell is one capable of undergoing proliferation in response to activation of the adrenergic receptor. In one specific embodiment of the foregoing, the adrenergic receptor includes a mutation in the third cytoplasmic loop thereof which renders the adrenergic receptor constitutively active, and the host cell undergoes proliferation in response to the constitutively active adrenergic receptor. Also disclosed are in vitro assays employing the foregoing which are useful for screening test compounds for antitumor and antiatherogenic activity, along with a diagnostic assay for detecting the oncogenic activation of cells in a patient. The diagnostic assay comprises collecting sample cells which express adrenergic receptors from the patient, and then detecting the presence or absence of a mutation in the adrenergic receptor which renders the receptor constitutively active. The presence of such a mutation indicates the oncogenic activation of the cells.
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