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Updated: Aug 23, 2026

A Facile Protocol to Generate Site-Specifically Acetylated Proteins in Escherichia Coli
Published on: December 9, 2017
Acetylation of proteins as novel target for antitumor therapy: review article
E Di Gennaro1, F Bruzzese, M Caraglia
1Dipartimento di Oncologia Sperimentale, Istituto Nazionale Tumori Fondazione G. Pascale, Napoli, Italy.
Abstract:
Imbalance in histone acetylation can lead to changes in chromatin structure and transcriptional dysregulation of genes that are involved in the control of proliferation, cell-cycle progression, differentiation and/or apoptosis. Histone acetyltransferases (HATs) and histone deacetylases (HDACs), are two classes of enzymes regulating histone acetylation and whose altered activity has been identified in several cancers. HATs and HDACs enzymes also target non histone protein substrates, including transcription factors, nuclear import factors, cytoskeleton and chaperon proteins. HDAC inhibitors are a novel class of anticancer agents which have been recently shown to induce growth arrest and apoptosis in a variety of human cancer cells by mechanism that cannot be solely attributed to the level of histone acetylation. Several clinical studies with HDAC inhibitors are ongoing, however the molecular basis for their tumour selectivity remains unknown and represent a challenge for the cancer research community.
Insights
Histone deacetylase (HDAC) inhibitors show promise as anticancer agents by inducing cancer cell apoptosis. However, the precise mechanisms behind their tumor selectivity are still under investigation, posing a challenge for cancer research.
Area of Science:
- Molecular Biology
- Biochemistry
- Cancer Research
Background:
- Histone acetylation regulates gene expression, impacting cell proliferation, differentiation, and apoptosis.
- Aberrant activity of histone acetyltransferases (HATs) and histone deacetylases (HDACs) is implicated in various cancers.
- HDACs and HATs also modify non-histone proteins, affecting diverse cellular processes.
Purpose of the Study:
- To explore the anticancer potential of HDAC inhibitors.
- To investigate the mechanisms underlying HDAC inhibitor-induced cancer cell apoptosis and growth arrest.
- To address the challenge of understanding the molecular basis for tumor selectivity of HDAC inhibitors.
Main Methods:
- Review of existing literature on HDAC inhibitors and their mechanisms of action.
- Analysis of clinical studies involving HDAC inhibitors.
- Exploration of the role of histone acetylation and non-histone protein targets.
Main Results:
- HDAC inhibitors demonstrate efficacy in inducing growth arrest and apoptosis in diverse human cancer cells.
- The observed anti-cancer effects cannot be solely explained by changes in histone acetylation.
- Ongoing clinical trials are evaluating the therapeutic potential of these agents.
Conclusions:
- HDAC inhibitors represent a promising class of novel anticancer agents.
- Further research is needed to elucidate the molecular mechanisms, particularly tumor selectivity, of HDAC inhibitors.
- Understanding these mechanisms is crucial for advancing cancer therapy.
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