Deacetylases are enzymes that remove acetyl groups from protein substrates. HDACs are the most well studied deacetylases, which have the ability of opposing the effects of histone acetyltransferases (HATs) and restoring the positive charge of the histone tail lysine residue. Removal of the acetyl group leads to a more tightly compacted, heterochromatin conformation, thereby negatively regulating gene expression.
So far, it has been already identified at least 4 classes of HDACs. Class I HDACs include 1, 2, 3, and 8. Class II HDACs contain 4, 5, 6, 7, 9, and 10. Class III enzymes, known as sirtuins, include SIRTs 1-7. The Class IV enzyme contains only HDAC11, which has features of both Class I and II. HDACs are tightly participated in cell cycle regulation, cell proliferation, and in the development of human diseases including cancers, neurological diseases, cardiovascular and pulmonary diseases. By detection of the activity and inhibition of HDACs, it is important in elucidating mechanisms of epigenetic regulation of gene activation and silencing, and also benefiting cancer diagnostics and therapeutics.
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Jeu 23 Aoû 2018 - 9:31