Data on Gene and Protein Expression Changes Induced by Apabetalone (RVX-208) in Ex Vivo Treated Human Whole Blood and Primary Hepatocytes

Overview

Journal Data Brief

Date 2016 Aug 30

PMID 27570805

Citations 5

Authors

Sylwia Wasiak

Dean Gilham

Laura M Tsujikawa

Christopher Halliday

Karen Norek

Reena G Patel

Kevin G McLure

Peter R Young

Allan Gordon

Ewelina Kulikowski

Jan Johansson

Michael Sweeney

Norman C Wong

Affiliations

Soon will be listed here.

Abstract

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 Cardiovascular Disease" (Gilham et al., 2016) [1]. It shows that RVX-208 and a comparator BET inhibitor (BETi) JQ1 increase mRNA expression and production of apolipoprotein A-I (ApoA-I), the main protein component of high density lipoproteins, in primary human and African green monkey hepatocytes. In addition, reported here are gene expression changes from a microarray-based analysis of human whole blood and of primary human hepatocytes treated with RVX-208.

Citing Articles

The Bromodomain and Extraterminal Protein Inhibitor Apabetalone Ameliorates Kidney Injury in Diabetes by Regulating Cholesterol Accumulation and Modulating the Gut Microbiota.

Wang M, Huang Z, Zhu Y, Li X, Sun H, Fan Q Kidney Int Rep. 2025; 10(2):522-534.

PMID: 39990894 PMC: 11843129. DOI: 10.1016/j.ekir.2024.11.022.

Reduction in the risk of major adverse cardiovascular events with the BET protein inhibitor apabetalone in patients with recent acute coronary syndrome, type 2 diabetes, and moderate to high likelihood of non-alcoholic fatty liver disease.

Toth P, Schwartz G, Nicholls S, Khan A, Szarek M, Ginsberg H Am J Prev Cardiol. 2022; 11:100372.

PMID: 36039183 PMC: 9419281. DOI: 10.1016/j.ajpc.2022.100372.

Apabetalone and hospitalization for heart failure in patients following an acute coronary syndrome: a prespecified analysis of the BETonMACE study.

Nicholls S, Schwartz G, Buhr K, Ginsberg H, Johansson J, Kalantar-Zadeh K Cardiovasc Diabetol. 2021; 20(1):13.

PMID: 33413345 PMC: 7791841. DOI: 10.1186/s12933-020-01199-x.

Epigenetic Modulation by Apabetalone Counters Cytokine-Driven Acute Phase Response , in Mice and in Patients with Cardiovascular Disease.

Wasiak S, Gilham D, Daze E, Tsujikawa L, Halliday C, Stotz S Cardiovasc Ther. 2020; 2020:9397109.

PMID: 32821285 PMC: 7416228. DOI: 10.1155/2020/9397109.

Effect of Apabetalone Added to Standard Therapy on Major Adverse Cardiovascular Events in Patients With Recent Acute Coronary Syndrome and Type 2 Diabetes: A Randomized Clinical Trial.

Ray K, Nicholls S, Buhr K, Ginsberg H, Johansson J, Kalantar-Zadeh K JAMA. 2020; 323(16):1565-1573.

PMID: 32219359 PMC: 7101505. DOI: 10.1001/jama.2020.3308.

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