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

Nazanin Zohourian, James A.L. Brown

Research output: Contribution to journalArticlepeer-review

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.

Original languageEnglish
Pages (from-to)671-80
Number of pages10
JournalEpigenomics
Volume16
Issue number9
DOIs
Publication statusPublished - 2024

Keywords

  • acetyltransferase
  • cancer
  • epigenetic
  • HAT
  • inhibitor
  • KAT
  • lysine
  • precision
  • small molecule
  • targeted
  • therapeutic

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