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Review

Biochemical aspects of chromatin-modifying drugs.

Aug 2026 · Drug Discovery Today · Vol 31, pp. 104784 · 0 citations · 59 references
Medicine

TL;DR

The present review provides an overview of the biochemical and pharmacological mechanisms of chromatin-modifying drugs, and some downstream effects of the aforementioned chromatin-modifying drugs.

Abstract

Epigenomic dysregulation is associated with several noncommunicable diseases (NCDs). Chromatin-modifying drugs have the ability to re-establish normal epigenetic regulation, thereby fine-tuning the epigenome. The biochemical and pharmacological mechanisms of these drugs, which target histone lysine and arginine methyltransferases, DNA methyltransferases, histone deacetylases and histone acetyltransferases, histone demethylases and bromodomain and extra-terminal motifs, serve as ideal tools for understanding the modes of action of these epigenetic regulators and the resulting biological events within chromatin. The present review provides an overview of these biochemical mechanisms and some downstream effects of the aforementioned chromatin-modifying drugs.

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