[Assay for inhibitory activity of histone deacetylase].
Recently, it has become clearer that abnormal epigenetics is profoundly involved in many human diseases. Histone acetylation is one of the important mechanisms by which epigenetics is controlled. Reversible histone acetylation, which occurs at conserved lysine residues clustered near the amino-terminus of core histones, mediates changes in nucleosome conformation and transcriptional activity. Acetylation and deacetylation are catalyzed by specific enzyme families, histone acetyltransferases (HATs) and deacetylases (HDACs), respectively. Since aberrant histone acetylation has been linked to malignant diseases in some cases, HDAC inhibitors bear great potential as new drugs due to their ability to modulate transcription and to induce differentiation and apoptosis. Some of the HDAC inhibitors are currently under clinical investigations. Therefore, HDAC has been considered as a molecular target for cancer therapy. We are providing a service for evaluating the HDAC inhibitory activity of compounds that are sent to the screening committee.
Yoshida
Minoru
M
Chemical Genetics Laboratory, Discovery Research Institute, RIKEN, CREST, JST, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan.
D000107:Acetylation; D000123:Acetyltransferases / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D051548:Histone Acetyltransferases; D056572:Histone Deacetylase Inhibitors; D006655:Histone Deacetylases / Q000378:metabolism* / Q000502:physiology; D006801:Humans; D009369:Neoplasms / Q000201:enzymology* / Q000628:therapy; D015398:Signal Transduction
D004791:Enzyme Inhibitors; D056572:Histone Deacetylase Inhibitors; D000123:Acetyltransferases; D051548:Histone Acetyltransferases; D006655:Histone Deacetylases