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YF343, A Novel Histone Deacetylase Inhibitor, Combined with CQ to Inhibit- Autophagy, Contributes to Increased

Na Liu1, Tingting Luo1, Jing Zhang1

  • 1School of Biological Science and Technology, University of Jinan, Jinan 250022, China.

Current Medicinal Chemistry
|January 23, 2023
PubMed
Abstract

Insights

This study shows that the novel histone deacetylase inhibitor YF-343 effectively targets triple-negative breast cancer. Combining YF-343 with chloroquine, an autophagy inhibitor, significantly enhances its anticancer effects by overcoming pro-survival autophagy.

Area of Science:

  • Oncology
  • Molecular Biology
  • Epigenetics

Background:

  • Epigenetic modifications are crucial in cancer development.
  • Histone deacetylase inhibitors (HDACis) are promising anticancer agents.
  • Triple-negative breast cancer (TNBC) requires novel therapeutic strategies.

Purpose of the Study:

  • To evaluate the anticancer efficacy of YF-343, a novel hydroxamate-based HDACi, in TNBC.
  • To elucidate the underlying mechanisms of YF-343 action, including its effect on autophagy.
  • To explore combination therapy strategies for TNBC.

Main Methods:

  • YF-343 identified as a novel HDACi using a drug screening kit.
  • Biological effects assessed via Western blot and flow cytometry in breast cancer cell lines.
  • Mechanism of action investigated using gene expression profiling, qPCR, ChIP assays, and more.

Main Results:

  • YF-343 demonstrated significant cytotoxicity, apoptosis induction, and cell cycle arrest in TNBC cells.
  • YF-343 induced autophagy, a pro-survival mechanism in cancer cells.
  • Combination of YF-343 with autophagy inhibitor chloroquine (CQ) markedly suppressed tumor progression in vitro and in vivo.

Conclusions:

  • YF-343 exhibits anticancer activity in TNBC by modulating epigenetic events and inducing autophagy.
  • The transcription factor E2F7 plays a role in YF-343-induced autophagy.
  • Combination therapy with YF-343 and CQ presents a promising strategy for breast cancer treatment.
Keywords:
E2F7HDACiapoptosisautophagychloroquinetriple-negative breast cancer

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