A Review on Important Histone Acetyltransferase (HAT) Enzymes as Targets for Cancer Therapy

Author(s): Mohammad Ghanbari, Reza Safaralizadeh*, Kiyanoush Mohammadi.

Journal Name: Current Cancer Therapy Reviews

Volume 15 , Issue 2 , 2019

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Graphical Abstract:


At the present time, cancer is one of the most lethal diseases worldwide. There are various factors involved in the development of cancer, including genetic factors, lifestyle, nutrition, and so on. Recent studies have shown that epigenetic factors have a critical role in the initiation and development of tumors. The histone post-translational modifications (PTMs) such as acetylation, methylation, phosphorylation, and other PTMs are important mechanisms that regulate the status of chromatin structure and this regulation leads to the control of gene expression. The histone acetylation is conducted by histone acetyltransferase enzymes (HATs), which are involved in transferring an acetyl group to conserved lysine amino acids of histones and consequently increase gene expression. On the basis of similarity in catalytic domains of HATs, these enzymes are divided into different groups such as families of GNAT, MYST, P300/CBP, SRC/P160, and so on. These enzymes have effective roles in apoptosis, signaling pathways, metastasis, cell cycle, DNA repair and other related mechanisms deregulated in cancer. Abnormal activation of HATs leads to uncontrolled amplification of cells and incidence of malignancy signs. This indicates that HAT might be an important target for effective cancer treatments, and hence there would be a need for further studies and designing of therapeutic drugs on this basis. In this study, we have reviewed the important roles of HATs in different human malignancies.

Keywords: Epigenetics, histone modification, histone acetyltransferase, cancer, drug design, post-translational modifications.

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Year: 2019
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DOI: 10.2174/1573394714666180720152100
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