منابع مشابه
Rvx 208
RVX 208 (RVX-208; RVX000222) is a first-in-class novel small molecule in development by Resverlogix Corporation for acute coronary syndromes, atherosclerosis and Alzheimer disease. It increases the levels of apolipoprotein A1 and high-density lipoprotein cholesterol, thereby potentially reducing the risk for cardiovascular disease. This review discusses the key development milestones and therap...
متن کاملRVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain.
Bromodomains have emerged as attractive candidates for the development of inhibitors targeting gene transcription. Inhibitors of the bromo and extraterminal (BET) family recently showed promising activity in diverse disease models. However, the pleiotropic nature of BET proteins regulating tissue-specific transcription has raised safety concerns and suggested that attempts should be made for do...
متن کاملRVX-208, an Inducer of ApoA-I in Humans, Is a BET Bromodomain Antagonist
Increased synthesis of Apolipoprotein A-I (ApoA-I) and HDL is believed to provide a new approach to treating atherosclerosis through the stimulation of reverse cholesterol transport. RVX-208 increases the production of ApoA-I in hepatocytes in vitro, and in vivo in monkeys and humans, which results in increased HDL-C, but the molecular target was not previously reported. Using binding assays an...
متن کاملDownregulation of the Complement Cascade In Vitro, in Mice and in Patients with Cardiovascular Disease by the BET Protein Inhibitor Apabetalone (RVX-208)
Apabetalone (RVX-208) is an epigenetic regulator developed to treat cardiovascular disease (CVD) that targets BET proteins. Through transcriptional regulation RVX-208 modulates pathways that underlie CVD including reverse cholesterol transport, vascular inflammation, coagulation, and complement. Using transcriptomics and proteomics we show that complement is one of the top pathways downregulate...
متن کاملData on gene and protein expression changes induced by apabetalone (RVX-208) in ex vivo treated human whole blood and primary hepatocytes
Apabetalone (RVX-208) inhibits the interaction between epigenetic regulators known as bromodomain and extraterminal (BET) proteins and acetyl-lysine marks on histone tails. Data presented here supports the manuscript published in Atherosclerosis "RVX-208, a BET-inhibitor for Treating Atherosclerotic Cardiovascular Disease, Raises ApoA-I/HDL and Represses Pathways that Contribute to Cardiovascul...
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ژورنال
عنوان ژورنال: Journal of the American College of Cardiology
سال: 2010
ISSN: 0735-1097
DOI: 10.1016/j.jacc.2010.02.035