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Assays for Validating Histone Acetyltransferase Inhibitors
09:11

Assays for Validating Histone Acetyltransferase Inhibitors

Published on: August 6, 2020

A work in progress: the clinical development of histone deacetylase inhibitors

Silvia Marsoni1, Giovanna Damia, Gabriella Camboni

  • 1SENDO Foundation, Milano, Italy. marsonis@sendo-org.it

Epigenetics
|May 20, 2008
PubMed

Insights

Histone deacetylase inhibitors (HDACIs) show promise in oncology by affecting cell functions and protein acetylation. This review discusses their clinical development, challenges, and strategies for solid tumors.

Area of Science:

  • Oncology
  • Epigenetics
  • Pharmacology

Background:

  • Histone deacetylases (HDAC) are recognized oncology targets.
  • HDAC inhibitors (HDACIs) modulate diverse cellular functions like apoptosis and angiogenesis.
  • HDACIs affect epigenetic regulation and other acetylation-dependent processes in cancer cells.

Purpose of the Study:

  • To review the clinical development of HDACIs in oncology.
  • To discuss challenges in HDACIs' clinical translation.
  • To emphasize spectrum of activity, solid tumor strategies, cardiac effects, and biomarkers.

Main Methods:

  • Literature review of preclinical and clinical studies on HDACIs in oncology.
  • Analysis of clinical trial data and outcomes.
  • Discussion of current challenges and future directions for HDACIs.

Main Results:

  • HDACIs demonstrate broad preclinical activity affecting multiple cancer hallmarks.
  • Clinical development faces challenges including defining optimal use in solid tumors.
  • Cardiac side effects and biomarker identification are critical areas for investigation.

Conclusions:

  • HDACIs represent a promising class of epigenetic drugs in oncology.
  • Addressing clinical development challenges is crucial for successful therapeutic application.
  • Further research on efficacy, safety, and predictive biomarkers is warranted for HDACIs.

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