Inhibitors of Histone Deacetylases

Histone Deacetylases and their Inhibitors as Potential

treatment regimen is still an unmet need. This might lead to the fact that few CCA patients are suitable for the surgery as well as the limitation of other therapeutic modalities (Patel, 2006; Sia et al., 2013; Zabron et al., 2013). In addition, the palliative chemotherapy and radiotherapy have been used as adjuvant therapy for this cancer type. Various chemotherapeutic agents e.g. 5-fluorourac...

Dual Inhibitors Against Topoisomerases and Histone Deacetylases

Topoisomerases and histone deacetylases (HDACs) are considered as important therapeutic targets for a wide range of cancers, due to their association with the initiation, proliferation and survival of cancer cells. Topoisomerases are involved in the cleavage and religation processes of DNA, while HDACs regulate a dynamic epigenetic modification of the lysine amino acid on various proteins. Exte...

Developing selective histone deacetylases (HDACs) inhibitors through ebselen and analogs

Histone deacetylases (HDACs) are key regulators of gene expression in cells and have been investigated as important therapeutic targets for cancer and other diseases. Different subtypes of HDACs appear to play disparate roles in the cells and are associated with specific diseases. Therefore, substantial effort has been made to develop subtype-selective HDAC inhibitors. In an effort to discover ...

Histone Deacetylases Inhibit IFN-

Chemical Phylogenetics of Histone Deacetylases

The broad study of histone deacetylases in chemistry, biology and medicine relies on tool compounds to derive mechanistic insights. A phylogenetic analysis of class I and II histone deacetylases (HDACs) as targets of a comprehensive, structurally diverse panel of inhibitors revealed unexpected isoform selectivity even among compounds widely perceived as nonselective. The synthesis and study of ...