Aberrant expression of epigenetic regulators of gene expression contributes to initiation and progression of cancer. During recent years, considerable research efforts have focused on the role of histone acetyltransferases (HATs) and histone deacetylases (HDACs) in cancer cells, and the identification of pharmacologic agents that modulate gene expression via inhibition of HDACs. The following r...

Rates of histone acetylation and deacetylation in nuclei from fetal, adult, and two kinds of neoplastic rat hepatocytes were examined. Histone acetylation in isolated nuclei was measured in the presence of 6 mM sodium n-butyrate, a potent inhibitor of deacetylase, and in the absence of the inhibitor. The deacetylase activity was estimated from the difference between the rates with or without th...

Histone-modifying proteins have been identified as promising targets to treat several diseases including cancer and parasitic ailments. In silico methods incorporated within a variety of drug discovery programs facilitate the identification development novel lead compounds. this study, we explore binding modes series benzhydroxamates derivatives developed histone deacetylase inhibitors Schistos...

Histone deacetylases (HDACs) are non-redundant chromatin-modifying enzymes that are critical cellular regulators and are often overexpressed in cancers. Targeting them by HDAC inhibitors (HDACis) can induce growth arrest, differentiation or apoptosis, making HDACi agents promising anti-cancer drugs, and these are currently being tested in clinical trials. Specific roles of the individual HDAC i...

Histone deacetylase inhibitors represent a promising new class of compounds for the treatment of cancer. Inhibitors of this kind currently under clinical evaluation mainly target the classical (Rpd3/Hda1) family of histone deacetylases. Of particular note, the U.S. Food and Drug Administration recently approved the first histone deacetylase inhibitor (Zolinza: Merck and Co., Whitehouse Station,...

Histone deacetylases are set of enzymes that have been of interest in drug discovery for the last more than 3 decades. They are responsible for cleaving of acetyl groups from acetyl-lysine residues in histones and various non-histone proteins. Histone deacetylase inhibition is a contemporary, clinically validated therapeutic tactic for cancer treatment. Hydroxamic acid derivatives are among the...

BACKGROUND Fibroblast growth factor 21, a novel regulator of glucose and lipid metabolism, has robust protective properties in neurons. However, its expression and function in glia are unknown. Valproic acid, a mood stabilizer and anticonvulsant, is a histone deacetylase inhibitor and a dynamic gene regulator. We investigated whether histone deacetylase inhibition by valproic acid and other inh...

Title:Suberoylanilide hydroxamic acid, an inhibitor of histone deacetylase, suppresses vasculogenic mimicry and proliferation of highly aggressive pancreatic cancer PaTu8988 cells

Neuroblastoma is a childhood cancer, which spontaneously regresses. This has led to a search for agents that mimic this process. We show that both natural and synthetic ligands of PPARgamma (peroxisome-proliferator-activated receptor gamma) inhibit the growth of neuroblastoma cells in vitro. The degree of PPAR activation was attenuated however in the presence of the retinoblastoma protein. Addi...