Histone deacetylase (Pan-HDAC) (Pan-HDAC)

Pan-histone deacetylases (Pan-HDACs) represent a family of enzymes that regulate gene expression by removing acetyl groups from lysine residues on histones and other cellular proteins (PMID: 22421968). This enzymatic activity leads to a more condensed chromatin structure, typically resulting in transcriptional repression of various genes, including those involved in cell cycle control and apoptosis (PMID: 30107119). In many cancers, HDACs are dysregulated, leading to the epigenetic silencing of tumor suppressor genes, which facilitates tumor progression and survival (PMID: 28231530). Pan-HDAC inhibitors are therapeutic agents designed to inhibit multiple HDAC isoforms—primarily across Class I, II, and IV—thereby restoring normal acetylation levels and inducing anti-tumor effects such as growth arrest and cell death (PMID: 25813451). While these inhibitors have shown significant clinical efficacy in hematological malignancies like cutaneous T-cell lymphoma and multiple myeloma, their broad activity profile is often associated with systemic toxicities, including myelosuppression and gastrointestinal distress (PMID: 21358717). Recent clinical developments have also expanded the use of Pan-HDAC inhibitors into non-oncological indications, such as Duchenne muscular dystrophy (PMID: 38513465).

Other names

HDAC familyHistone deacetylasesLysine deacetylasesKDACsZinc-dependent histone deacetylases

Inhibition of zinc-dependent histone deacetylase enzymes (Classes I, II, and IV), leading to increased acetylation of histone and non-histone proteins, remodeling of chromatin, and modulation of gene expression patterns associated with cell cycle arrest and apoptosis (PMID: 25813451).