Bromodomain and Extra-Terminal Protein Inhibition in Atherosclerosis: Advantages and Disappointments

Alexander E. Berezin, Alexander A. Berezin


Major cardiovascular events (MACEs) are leading cause of premature death in general population, as well as in the patients with known atherosclerosis and coronary artery disease (CAD). Manifestation and progression of atherosclerosis is tightly related to systemic and local microvascular inflammation that accelerate vascular remodeling, triggers endothelial dysfunction and promote negative impact of the dyslipidemia on the vasculature. The bromodomain and extra terminal (BET) proteins were first proposed as anticancer drugs and then cardio and vascular protective effects were found. The aim of the mini review is summarize knowledge for BET protein inhibitors in prevention of poor clinical outcomes in patients with atherosclerosis and CAD. The results of pool analysis of some clinical trials, such as ASSERT, ASSURE-I, SUSTAIN, are disputed. It has been shown positive effects of apabetalone on the levels of Apo A-I and high-density lipoprotein cholesterol that was associated with significant declining of the systemic and local inflammatory reaction. There is evidence regarding that the apabetalone induced reverse of the atherosclerotic plaque volume.


Atherosclerosis; Coronary artery disease; Dyslipidemia; inflammation; Bromodomain and extra terminal proteins

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