Inhibition of histone deacetylases.
Reversible histone acetylation, governed dynamically by histone acetyltransferases (HATs) and histone deacetylases (HDACs), plays a pivotal role in regulation of gene expression through remodeling chromatin structure. Manipulation of the equilibrium between acetylation and deacetylation of histones by specific HDAC inhibitors is thus a useful tool to study functional role(s) for histone hyper-/hypoacetylation in controlling gene transcription and many other cellular activities. By using the trans-activating effect of trichostatin A (TSA), a widely used HDAC inhibitor, on the telomerase reverse transcriptase (hTERT) gene as an example, we summarize various aspects of HDAC inhibitors and provide a general strategy for their in vitro application in studies of gene regulation.
Liu
Cheng
C
Department of Medicine, Division of Hematology, Karolinska Hospital, Stockholm, Sweden.
Xu
Dawei
D
D000107:Acetylation; D000818:Animals; D015153:Blotting, Western; D002478:Cells, Cultured; D042002:Chromatin Assembly and Disassembly; D004268:DNA-Binding Proteins; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D056572:Histone Deacetylase Inhibitors; D006657:Histones / Q000302:isolation & purification / Q000378:metabolism; D006801:Humans; D006877:Hydroxamic Acids / Q000494:pharmacology*; D051379:Mice; D008967:Molecular Biology / Q000379:methods*; D051381:Rats; D013601:T-Lymphocytes / Q000187:drug effects; D019098:Telomerase / Q000187:drug effects / Q000235:genetics
D004268:DNA-Binding Proteins; D004791:Enzyme Inhibitors; D056572:Histone Deacetylase Inhibitors; D006657:Histones; D006877:Hydroxamic Acids; C012589:trichostatin A; D019098:Telomerase