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Review
. 2024 Apr 19;16(9):671-680.
doi: 10.2217/epi-2023-0443. Online ahead of print.

Current trends in clinical trials and the development of small molecule epigenetic inhibitors as cancer therapeutics

Nazanin Zohourian  1 , James Al Brown  1   2   3   4
Affiliations
Review

Current trends in clinical trials and the development of small molecule epigenetic inhibitors as cancer therapeutics

Nazanin Zohourian et al. Epigenomics. .

Abstract

Epigenetic mechanisms control and regulate normal chromatin structure and gene expression patterns, with epigenetic dysregulation observed in many different cancer types. Importantly, epigenetic modifications are reversible, offering the potential to silence oncogenes and reactivate tumor suppressors. Small molecule drugs manipulating these epigenetic mechanisms are at the leading edge of new therapeutic options for cancer treatment. The clinical use of histone deacetyltransferases inhibitors (HDACi) demonstrates the effectiveness of targeting epigenetic mechanisms for cancer treatment. Notably, the development of new classes of inhibitors, including lysine acetyltransferase inhibitors (KATi), are the future of epigenetic-based therapeutics. We outline the progress of current classes of small molecule epigenetic drugs for use against cancer (preclinical and clinical) and highlight the potential market growth in epigenetic-based therapeutics.

Keywords: HAT; KAT; acetyltransferase; cancer; epigenetic; inhibitor; lysine; precision; small molecule; targeted; therapeutic.

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Conflict of interest statement

The authors have no competing interests or relevant affiliations with any organization or entity with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Figures

Figure 1.
Figure 1.
Global epigenetics drugs market growth. Values collated from [46,47].
Figure 2.
Figure 2.
Epigenetic targets, classes of epigenetic small molecule inhibitors and drug-development pipeline.
See this image and copyright information in PMC

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