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Updated: Jun 22, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
09:11

Assays for Validating Histone Acetyltransferase Inhibitors

Published on: August 6, 2020

Targeting histone deacetylases for heart failure

Erik W Bush1, Timothy A McKinsey

  • 1Gilead Colorado, Inc., 3333 Walnut Street, Boulder, Colorado 80301, USA. erik.bush@gilead.com

Expert Opinion on Therapeutic Targets
|May 27, 2009
PubMed

Insights

Histone deacetylases (HDACs) are promising therapeutic targets for heart failure. Further research is needed to validate HDAC-directed therapies, considering their non-cardiac roles.

Area of Science:

  • Cardiovascular Biology
  • Molecular Medicine
  • Pharmacology

Background:

  • Cardiac remodeling, involving myocyte hypertrophy, death, and fibrosis, is triggered by stresses like hypertension and myocardial infarction, leading to heart failure.
  • Recent research implicates histone deacetylases (HDACs) in regulating pathological cardiac remodeling processes.

Purpose of the Study:

  • To review target validation experiments for HDACs in the context of heart failure.
  • To highlight the non-cardiac functions of HDACs that require consideration for developing effective therapies.

Main Methods:

  • Literature review of existing studies on HDACs and cardiac remodeling.
  • Analysis of HDACs' roles in pathological signaling pathways.

Main Results:

  • HDACs are positioned downstream in pathological signaling cascades relevant to heart failure.
  • HDACs represent attractive therapeutic targets due to their role in disease progression.

Conclusions:

  • HDACs are unique and attractive therapeutic targets for heart failure.
  • In vivo proof-of-concept testing with novel small molecule regulators is crucial to confirm the validity and viability of HDAC-directed approaches.
Abstract

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