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Assays for Validating Histone Acetyltransferase Inhibitors
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Assays for Validating Histone Acetyltransferase Inhibitors

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Histone deacetylase inhibitor based prodrugs

Wenli Fan1, Lihui Zhang2, Qixao Jiang3

  • 1Department of Medicinal Chemistry, School of Pharmacy, Weifang Medical University, Weifang, Shandong, China.

European Journal of Medicinal Chemistry
|July 18, 2020
PubMed

Insights

Prodrug strategies enhance histone deacetylase inhibitors (HDACIs) for cancer therapy. This approach improves drug properties like solubility and tumor targeting, creating promising anticancer drug candidates.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Oncology

Background:

  • Histone deacetylases (HDACs) are crucial enzymes in cancer development.
  • HDAC inhibitors (HDACIs) are a therapeutic strategy with FDA-approved drugs.
  • Current HDACIs face limitations in physicochemical properties, selectivity, and potency.

Purpose of the Study:

  • To summarize the development of HDACI-based prodrugs.
  • To explore strategies for improving HDACI clinical potential.
  • To guide structural modifications for enhanced anticancer drug candidates.

Main Methods:

  • Review of prodrug strategies applied to HDACIs.
  • Analysis of studies reporting improvements in HDACI properties.
  • Summary of different types of HDACI-based prodrugs.

Main Results:

  • Prodrug strategies can enhance stability, solubility, lipophilicity, and oral bioavailability of HDACIs.
  • Prodrugs can improve tumor cell selectivity.
  • Various prodrug designs have been reported for HDACIs.

Conclusions:

  • Prodrug strategies offer a viable approach to overcome limitations of current HDACIs.
  • HDACI-based prodrugs show high potential as future anticancer drug candidates.
  • Further structural modification of HDACIs via prodrugs is warranted.
Keywords:
Histone deacetylase inhibitorPhysicochemical propertyProdrugSelectivityStructural modification

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