Epigenetic modifications play central roles in cellular differentiation and their deregulations really
contribute to tumor development. Histone deacetylase (HDAC) enzymes can exert their functions in the
epigenetic regulation of gene expression related to oncogenesis via deacetylating the lysine residues of histones in
the chromatin and various non-histone proteins. A majority of HDAC inhibitors (HDACIs) have been in different
stages of preclinical and clinical trials with potent anticancer activity recently. Among these agents, chidamide
tested as either monotherapeutic agent or in combination regimens for numerous hematological and solid
malignancies has shown promising potential as an orally active subtype-selective HDACI. Herein we will
highlight the progress of clinical trials of chidamide and rationally analyze those results from both preclinical and
clinical studies about chidamide as an epigenetic modulator in cancer therapy.
Keywords: Epigenetic, histone deacetylase inhibitors, chidamide, hematologic and solid cancers, preclinical and clinical trials.
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