Histone de-acetylase inhibitors: a promising future for cancer treatment?

Le résumé fourni par la source

Histone de-acetylase proteins or lysine de-acetylases, represent a group of enzymes regulating DNA and gene expression by eliminating acetyl groups (de-acetylation) from lysine amino acids on histones and non-histone proteins. Histone de-acetylase functions normally by being involved in a series of cellular pathways like cell growth, cell cycle, signal transduction, notch signaling pathway and especially transcription.However, abnormal acetylation of histone tails becomes tumorigenic with the resulting transcriptional lesions disrupting the apoptotic program of cells leading to neoplasia. Interaction with the catalytic site and blocking substrate access of histone de-acetylases in proliferation of tumor cells, anti-neoplastic agents called histone de-acetylase inhibitors (HDIs) shift the balance by inducing cell-cycle arrest in G1, activation of differentiation programs and activation of death-receptor and intrinsic apoptotic pathways in neoplastic cells. HDIs anti-proliferative effect in down regulation of BMI1 and c-MYC protein levels has shown promising results in treatment of the incurable AML as well as silencing estrogen receptor alpha in prevention of breast cancer.

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