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Updated: Sep 6, 2025

Studying Triple Negative Breast Cancer Using Orthotopic Breast Cancer Model
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Studying Triple Negative Breast Cancer Using Orthotopic Breast Cancer Model

Published on: March 20, 2020

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HDAC Inhibitors for the Therapy of Triple Negative Breast Cancer

Cristina Maccallini1, Alessandra Ammazzalorso1, Barbara De Filippis1

  • 1Department of Pharmacy, University G. d'Annunzio of Chieti-Pescara, Via dei Vestini, 31, 66100 Chieti, Italy.

Pharmaceuticals (Basel, Switzerland)
|June 24, 2022
PubMed

Insights

Histone deacetylase inhibitors (HDACIs) show promise for treating triple-negative breast cancer (TNBC). New drug designs targeting specific HDACs or multiple targets offer potent activity against TNBC progression.

Area of Science:

  • Oncology
  • Epigenetics
  • Pharmacology

Background:

  • Triple-negative breast cancer (TNBC) presents a significant clinical challenge due to poor prognosis and limited treatment options.
  • Epigenetic alterations, particularly those involving histone deacetylases (HDACs), play a crucial role in TNBC development and progression.

Purpose of the Study:

  • To review the potential of histone deacetylase inhibitors (HDACIs) as a therapeutic strategy for TNBC.
  • To discuss pharmacophoric models and structural modifications of HDACIs for enhanced anti-TNBC activity.

Main Methods:

  • Review of current literature on HDACIs and their application in TNBC.
  • Analysis of pharmacophoric models and structural features of potent HDAC inhibitors.
  • Discussion of isoform-selective and polypharmacological approaches.

Main Results:

  • Single-agent HDACIs have shown disappointing clinical results in TNBC.
  • Recent advancements in drug design, including isoform selectivity and polypharmacology, highlight the potential of HDACIs.
  • Specific pharmacophoric models and structural modifications can lead to potent anti-TNBC compounds.

Conclusions:

  • HDACIs represent a promising therapeutic avenue for triple-negative breast cancer.
  • Targeted and polypharmacological HDAC inhibition strategies are crucial for overcoming TNBC.
  • Further research into novel HDACI designs is warranted for effective TNBC treatment.
Keywords:
anticancerbenzamidechimeric compoundshistone deacetylasehydroxamateinhibitortriple negative breast cancer

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