Small molecule HDAC inhibitors: Promising agents for breast cancer treatment

Meiling Huang1, Jian Zhang2, Changjiao Yan1

  • 1Department of Thyroid, Breast and Vascular Surgery, Xijing Hospital, The Fourth Military Medical University, Xi'an 710032, PR China.

Bioorganic Chemistry
|August 14, 2019
PubMed

Insights

Histone deacetylase inhibitors (HDACIs) show promise for breast cancer treatment, particularly in combination therapies. Further research and clinical trials are essential for developing novel HDACIs and advancing treatments.

Area of Science:

  • Oncology
  • Epigenetics
  • Pharmacology

Background:

  • Breast cancer is a leading cause of death globally, characterized by complex heterogeneity.
  • Epigenetic alterations, including those involving histone deacetylases (HDACs), are critical in cancer development.
  • HDAC inhibitors (HDACIs) are emerging as potential therapeutic agents for cancer treatment.

Purpose of the Study:

  • To review the mechanisms and classifications of HDACs and HDACIs.
  • To explore the association between HDACs and breast cancer.
  • To summarize the structure-activity relationships, pharmacokinetics, toxicology, and clinical studies of HDACIs in breast cancer.

Main Methods:

  • Literature review of HDACs, HDACIs, and their role in breast cancer.
  • Analysis of structure-activity relationships (SAR) of HDACIs.
  • Compilation of data from registered clinical studies for breast cancer treatment.

Main Results:

  • HDACIs demonstrate efficacy in breast cancer treatment, especially when combined with other agents.
  • Significant research exists on HDACIs, including their classification, SAR, and properties.
  • Clinical studies indicate the potential of HDACIs, with ongoing trials expected.

Conclusions:

  • HDACIs offer a promising therapeutic avenue for breast cancer.
  • Combination therapy involving HDACIs shows enhanced effects.
  • Future research should focus on novel HDACI development and large-scale clinical trials.

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