Histone deacetylase inhibitors: discovery and development as anticancer agents

2005/11/25 by Paul A. Marks, Milos Dokmanovic · 2 citations
Biochemistry, Genetics and Molecular Biology · Neuroscience · #Histone Deacetylase Inhibitors Research #Protein Degradation and Inhibitors #Nuclear Receptors and Signaling

paper · doi:10.1517/13543784.14.12.1497

openalex publication_date 2005/11/25 · openalex created_date 2025/10/10 · openalex updated_date 2026/07/15

Abstract

Histone deacetylase (HDAC) inhibitors are a new class of targeted anticancer agents. Several HDAC inhibitors are in clinical trials and have shown significant activity against a spectrum of both haematological and solid tumours at doses that are well tolerated by patients. HDACs and histone acetyltransferases can, by reversible acetylation, modify the structure and function of histones and proteins in transcription factor complexes, which are involved in the regulation of gene expression, as well as many non-histone proteins that are involved in regulating cell proliferation and cell death. HDAC inhibitors are a structurally diverse group of molecules; these agents selectively alter the expression of genes. HDAC inhibitors can induce cancer cell death, whereas normal cells are relatively resistant to HDAC inhibitor-induced cell death.

Citations

• Controlling the double helix
• A class of hybrid polar inducers of transformed cell differentiation inhibits histone deacetylases
• Physiological functions of thioredoxin and thioredoxin reductase
• The Sir2 Family of Protein Deacetylases
• Crystal structure of the nucleosome core particle at 2.8 Å resolution
• Histone deacetylase inhibitor selectively induces p21 WAF1 expression and gene-associated histone acetylation

Cited by

• Multiple roles of HDAC inhibition in neurodegenerative conditions
• Chromatin remodeling [wikipedia]