Histone Deacetylase Inhibitor in Cancer Therapy

Dear Colleagues,

Epigenetic alterations are able to determine a substantial change in the assets of gene expression patterns.

Modifications of methylation status occur in the genome, leading to silencing or over-expression of genes.

Histone acetylation substantially modifies the structure of the histone core, providing the DNA sequence the possibility of being accessible by the transcription factor at the promoter region of genes, leading to the transcription of the corresponding genome code.

Hypo-acetylation has been implicated in malignant transformations and tumor progression, thus characterizing the epi-genome profile of cancer cells.

Since the discovery of the antifungal antibiotic Trichostatin A and its ability to inhibit the histone deacetylase, several other HDACi (histone deacetylase inhibitors) have been newly synthetized.

Current research has shown that the inhibition of histone deacetylase is capable of restoring the expression of genes implicated in cell cycle blockade and cell death, thus improving classical chemotherapy by overcoming multiple drug resistance.

Histone deacetylase inhibitors have a high potential in cancer therapy and their mechanisms of action are not yet fully elucidated.

Dr. Pietro Di Fazio
Guest Editor

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