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Histone Deacetylases (HDAC)Transcriptional regulation in eukaryotes is a multilevel hierarchical process. It is becoming clear that chromatin structure (the complex of DNA, histones and other components that make up chromosomes) plays a crucial role in regulating gene expression, both in normal and cancer tissue. One of the important regulatory post-translational modifications of chromatin is the acetylation of its histone proteins. Although the details are complex, in general chromatin with acetylated histones forms an open (euchromatin) structure in which genes are active. Deacetylation of histones is associated with condensing chromatin to a more compact structure (heterochromatin) in which the genes are silenced. The enzymes which catalyse the deacetylation of histones (histone deacetylases, HDACs) are emerging as an important cancer target. Several cancer promoting mutations and chromosomal translocations result in repression of transcription through abnormal recruitment and activation of HDACs, leading to neoplastic transformation. This is the rationale for the development of HDAC inhibitors as a new therapeutic approach to cancer. Trials have shown the anti-proliferative effect of histone deacetylase inhibitors in cell culture, animal models and in humans with both haematological and solid tumours. TopoTarget is amongst the leaders in the area of HDAC inhibitor drug discovery and development which, in part, reflects the company's early recognition of the potential of chromatin control when applied to cancer drug discovery. Useful links :
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