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Updated: Jan 21, 2026

Studying Triple Negative Breast Cancer Using Orthotopic Breast Cancer Model
Published on: March 20, 2020
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.
Abstract:
Breast cancer, a heterogeneous disease, is the most frequently diagnosed cancer and the second leading cause of cancer-related death among women worldwide. Recently, epigenetic abnormalities have emerged as an important hallmark of cancer development and progression. Given that histone deacetylases (HDACs) are crucial to chromatin remodeling and epigenetics, their inhibitors have become promising potential anticancer drugs for research. Here we reviewed the mechanism and classification of histone deacetylases (HDACs), association between HDACs and breast cancer, classification and structure-activity relationship (SAR) of HDACIs, pharmacokinetic and toxicological properties of the HDACIs, and registered clinical studies for breast cancer treatment. In conclusion, HDACIs have shown desirable effects on breast cancer, especially when they are used in combination with other anticancer agents. In the coming future, more multicenter and randomized Phase III studies are expected to be conducted pushing promising new therapies closer to the market. In addition, the design and synthesis of novel HDACIs are also needed.
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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