Search Results - "Tsujikawa, Laura M"
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Breaking boundaries: Pan BETi disrupt 3D chromatin structure, BD2-selective BETi are strictly epigenetic transcriptional regulators
Published in Biomedicine & pharmacotherapy (01-08-2022)“…Bromodomain and extraterminal proteins (BETs) are more than just epigenetic regulators of transcription. Here we highlight a new role for the BET protein BRD4…”
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Apabetalone, a Clinical-Stage, Selective BET Inhibitor, Opposes DUX4 Target Gene Expression in Primary Human FSHD Muscle Cells
Published in Biomedicines (30-09-2023)“…Facioscapulohumeral dystrophy (FSHD) is a muscle disease caused by inappropriate expression of the double homeobox 4 (DUX4) gene in skeletal muscle, and its…”
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Apabetalone Downregulates Fibrotic, Inflammatory and Calcific Processes in Renal Mesangial Cells and Patients with Renal Impairment
Published in Biomedicines (01-06-2023)“…Epigenetic mechanisms are implicated in transcriptional programs driving chronic kidney disease (CKD). Apabetalone is an orally available inhibitor of…”
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The BET inhibitor apabetalone decreases neuroendothelial proinflammatory activation in vitro and in a mouse model of systemic inflammation
Published in Translational neuroscience (01-01-2023)“…Brain vascular inflammation is characterized by endothelial activation and immune cell recruitment to the blood vessel wall, potentially causing a breach in…”
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Epigenetic Modulation by Apabetalone Counters Cytokine-Driven Acute Phase Response In Vitro, in Mice and in Patients with Cardiovascular Disease
Published in Cardiovascular therapeutics (2020)“…Chronic systemic inflammation contributes to cardiovascular disease (CVD) and correlates with the abundance of acute phase response (APR) proteins in the liver…”
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Benefit of Apabetalone on Plasma Proteins in Renal Disease
Published in Kidney international reports (01-05-2018)“…Apabetalone, a small molecule inhibitor, targets epigenetic readers termed BET proteins that contribute to gene dysregulation in human disorders. Apabetalone…”
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Inhibition of epigenetic reader proteins by apabetalone counters inflammation in activated innate immune cells from Fabry disease patients receiving enzyme replacement therapy
Published in Pharmacology research & perspectives (01-06-2022)“…Fabry disease (FD) is a rare X‐linked disorder of lipid metabolism, characterized by the accumulation of globotriaosylceramide (Gb3) due to defective the…”
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Data on gene and protein expression changes induced by apabetalone (RVX-208) in ex vivo treated human whole blood and primary hepatocytes
Published in Data in brief (01-09-2016)“…Apabetalone (RVX-208) inhibits the interaction between epigenetic regulators known as bromodomain and extraterminal (BET) proteins and acetyl-lysine marks on…”
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RVX-208, a BET-inhibitor for treating atherosclerotic cardiovascular disease, raises ApoA-I/HDL and represses pathways that contribute to cardiovascular disease
Published in Atherosclerosis (01-04-2016)“…Abstract High density lipoproteins (HDL), through activity of the main protein component apolipoprotein A-I (ApoA-I), can reduce the risk of cardiovascular…”
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Apabetalone downregulates factors and pathways associated with vascular calcification
Published in Atherosclerosis (01-01-2019)“…Apabetalone is an inhibitor of bromodomain and extraterminal (BET) proteins. In clinical trials, apabetalone reduced the incidence of major adverse cardiac…”
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Epigenetic BET reader inhibitor apabetalone (RVX-208) counters proinflammatory aortic gene expression in a diet induced obesity mouse model and in human endothelial cells
Published in Atherosclerosis (01-01-2023)“…Obese patients are at risk for type 2 diabetes mellitus (T2DM) and cardiovascular disease (CVD). A lipid-rich diet promotes arterial changes by inducing…”
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Apabetalone (RVX-208) reduces vascular inflammation in vitro and in CVD patients by a BET-dependent epigenetic mechanism
Published in Clinical epigenetics (12-07-2019)“…Apabetalone (RVX-208) is a bromodomain and extraterminal protein inhibitor (BETi) that in phase II trials reduced the relative risk (RR) of major adverse…”
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Dual mechanism: Epigenetic inhibitor apabetalone reduces SARS-CoV-2 Delta and Omicron variant spike binding and attenuates SARS-CoV-2 RNA induced inflammation
Published in International immunopharmacology (01-04-2023)“…•Epigenetic inhibitor apabetalone reduces SARS-CoV-2 spike protein binding to ACE2 abundant human lung cells regardless of mutations in Delta and Omicron…”
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Downregulation of the Complement Cascade In Vitro, in Mice and in Patients with Cardiovascular Disease by the BET Protein Inhibitor Apabetalone (RVX-208)
Published in Journal of cardiovascular translational research (01-08-2017)“…Apabetalone (RVX-208) is an epigenetic regulator developed to treat cardiovascular disease (CVD) that targets BET proteins. Through transcriptional regulation…”
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Abstract 10591: Epigenetic BET Reader Inhibitor Apabetalone (RVX-208) Counters Proinflammatory Aortic Gene Expression in a Diet Induced Obesity Mouse Model
Published in Circulation (New York, N.Y.) (16-11-2021)“…IntroductionObesity increases the risk of type 2 diabetes (DM2) and cardiovascular disease (CVD), due to associated insulin resistance, dyslipidemia, high…”
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Abstract 14112: Apabetalone (RVX-208) Reduces ACE2 Expression in Human Cell Culture Systems, Which Could Attenuate SARS-CoV-2 Viral Entry
Published in Circulation (New York, N.Y.) (17-11-2020)“…IntroductionApabetalone is an orally available small molecule that affects gene transcription by inhibiting BET protein interactions with acetylated histones…”
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