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BET and HDAC inhibitors induce similar genes and biological effects and synergize to kill in Myc-induced murine lymphoma

Proceedings of the National Academy of Sciences - PNAS, 2014-07, Vol.111 (26), p.E2721-E2730

2014

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RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist

PloS one, 2013-12, Vol.8 (12), p.e83190

2013

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RVX-297, a BET Bromodomain Inhibitor, Has Therapeutic Effects in Preclinical Models of Acute Inflammation and Autoimmune Disease

Molecular pharmacology, 2017-12, Vol.92 (6), p.694-706

2017

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RVX-297- a novel BD2 selective inhibitor of BET bromodomains

Biochemical and biophysical research communications, 2016-08, Vol.477 (1), p.62-67

2016

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Design and Synthesis of LM146, a Potent Inhibitor of PB1 with an Improved Selectivity Profile over SMARCA2

ACS omega, 2021-08, Vol.6 (33), p.21327-21338

2021

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In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208)

European journal of medicinal chemistry, 2013-06, Vol.64, p.121-128

2013

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Synthesis of NVS-BPTF-1 and evaluation of its biological activity

Bioorganic & medicinal chemistry letters, 2021-09, Vol.47, p.128208-128208, Article 128208

2021

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RVX-208: A Small Molecule That Increases Apolipoprotein A-I and High-Density Lipoprotein Cholesterol In Vitro and In Vivo

Journal of the American College of Cardiology, 2010-06, Vol.55 (23), p.2580-2589

2010

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A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice

Atherosclerosis, 2014-09, Vol.236 (1), p.91-100

2014

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Design and Characterization of Novel Covalent Bromodomain and Extra-Terminal Domain (BET) Inhibitors Targeting a Methionine

Journal of medicinal chemistry, 2018-09, Vol.61 (18), p.8202-8211

2018

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Novel approaches to targeting BRD4

Drug discovery today. Technologies, 2017-06, Vol.24, p.19-24

2017

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The phytochemical piceatannol induces the loss of CBL and CBL-associated proteins

Molecular cancer therapeutics, 2009-03, Vol.8 (3), p.602-614

2009

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Discovery of a new chemical series of BRD4(1) inhibitors using protein-ligand docking and structure-guided design

Bioorganic & medicinal chemistry letters, 2015-07, Vol.25 (14), p.2818-2823

2015

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Synthesis of macrocyclic scaffolds suitable for diversity-oriented synthesis of macrolides

Tetrahedron, 2009-09, Vol.65 (39), p.8132-8138

2009

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Identification of Novel Macrocyclic Peptidase Substrates via On-Bead Enzymatic Cyclization

Journal of organic chemistry, 2003-10, Vol.68 (22), p.8459-8464

2003

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Stilbene analogs as inducers of apolipoprotein-I transcription

European journal of medicinal chemistry, 2010-05, Vol.45 (5), p.2018-2023

2010

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Di-, Tri-, and Tetravalent Dendritic Galabiosides That Inhibit Hemagglutination by Streptococcus suis at Nanomolar Concentration

Journal of the American Chemical Society, 1997-07, Vol.119 (30), p.6974-6979

1997

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RVX-208

Journal of the American College of Cardiology, 2010-06, Vol.55 (23), p.2580-2589

2010

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Interaction of the verotoxin 1B subunit with soluble aminodeoxy analogues of globotriaosyl ceramides

Biochemical journal, 2002-12, Vol.368 (Pt 3), p.769-776

2002

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Abstract LB-038: Preclinical development and clinical validation of a whole blood pharmacodynamic marker assay for the BET bromodomain inhibitor ZEN-3694 in metastatic castration-resistant prostate cancer (mCRPC) patients

Cancer research (Chicago, Ill.), 2017-07, Vol.77 (13_Supplement), p.LB-038-LB-038

2017

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Abstract LB-207: Preclinical characterization of ZEN-3694, a novel BET bromodomain inhibitor entering phase I studies for metastatic castration-resistant prostate cancer (mCRPC)

Cancer research (Chicago, Ill.), 2016-07, Vol.76 (14_Supplement), p.LB-207-LB-207

2016

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Abstract 5495: BET bromodomain inhibitors abrogate cell cycle progression and induces apoptosis in Myc-induced mouse lymphoma cells without affecting MYC transcription

Cancer research (Chicago, Ill.), 2014-10, Vol.74 (19_Supplement), p.5495-5495

2014

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BET and HDAC inhibitors induce similar genes and biological effects and synergize to kill in Myc-induced murine lymphoma

Proceedings of the National Academy of Sciences - PNAS, 2014-07, Vol.111 (26), p.9377-9377

2014

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Multistep solution-Phase parallel synthesis of spiperone analogues

Bioorganic & medicinal chemistry letters, 2000-11, Vol.10 (21), p.2435-2439

2000

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Abstract LB-92: RVX-2135 is a novel, orally bioavailable epigenetic BET inhibitor that synergizes with cytarabine and idarubicin to inhibit proliferation of acute myeloid leukemia cells

Cancer research (Chicago, Ill.), 2013-04, Vol.73 (8_Supplement), p.LB-92-LB-92

2013

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BET and HDAC inhibitors induce similar genes and biological effects and synergize to kill in Myc-induced murine lymphoma

RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist

RVX-297, a BET Bromodomain Inhibitor, Has Therapeutic Effects in Preclinical Models of Acute Inflammation and Autoimmune Disease

RVX-297- a novel BD2 selective inhibitor of BET bromodomains

Design and Synthesis of LM146, a Potent Inhibitor of PB1 with an Improved Selectivity Profile over SMARCA2

In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208)

Synthesis of NVS-BPTF-1 and evaluation of its biological activity

RVX-208: A Small Molecule That Increases Apolipoprotein A-I and High-Density Lipoprotein Cholesterol In Vitro and In Vivo

A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice

Design and Characterization of Novel Covalent Bromodomain and Extra-Terminal Domain (BET) Inhibitors Targeting a Methionine

Novel approaches to targeting BRD4

The phytochemical piceatannol induces the loss of CBL and CBL-associated proteins

Discovery of a new chemical series of BRD4(1) inhibitors using protein-ligand docking and structure-guided design

Synthesis of macrocyclic scaffolds suitable for diversity-oriented synthesis of macrolides

Identification of Novel Macrocyclic Peptidase Substrates via On-Bead Enzymatic Cyclization

Stilbene analogs as inducers of apolipoprotein-I transcription

Di-, Tri-, and Tetravalent Dendritic Galabiosides That Inhibit Hemagglutination by Streptococcus suis at Nanomolar Concentration

RVX-208

Interaction of the verotoxin 1B subunit with soluble aminodeoxy analogues of globotriaosyl ceramides

Abstract LB-038: Preclinical development and clinical validation of a whole blood pharmacodynamic marker assay for the BET bromodomain inhibitor ZEN-3694 in metastatic castration-resistant prostate cancer (mCRPC) patients

Abstract LB-207: Preclinical characterization of ZEN-3694, a novel BET bromodomain inhibitor entering phase I studies for metastatic castration-resistant prostate cancer (mCRPC)

Abstract 5495: BET bromodomain inhibitors abrogate cell cycle progression and induces apoptosis in Myc-induced mouse lymphoma cells without affecting MYC transcription

BET and HDAC inhibitors induce similar genes and biological effects and synergize to kill in Myc-induced murine lymphoma

Multistep solution-Phase parallel synthesis of spiperone analogues

Abstract LB-92: RVX-2135 is a novel, orally bioavailable epigenetic BET inhibitor that synergizes with cytarabine and idarubicin to inhibit proliferation of acute myeloid leukemia cells

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