Histone deacetylase (HDAC) inhibitors

Induce acetylation of the NH2 terminal tail of core histones allowing recruitment of transcription factor complexes and leads to derepression of transcription.

Result in accumulation of acetyl groups on histones, causing DNA uncoiling within chromatin structure and transcriptional activation of genes.

A class of drugs targeting enzymes involved in epigenetic regulation of gene expression.

Presently: vorinostat, belinostat, romidepsin amd panobinostat approved.

HDAC approved for relapsed or refractory hematological cancers, specifically peripheral and cutaneous T-cell lymphomas and multiple myeloma, and responses have been reported in relapsed or refractory aggressive non-Hodgkin’s lymphomas including diffuse large B-cell lymphoma, Hodgkin’s lymphoma, acute and myeloid leukemia.

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