Journal
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
Volume 17, Issue 6, Pages 802-812Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1871520616666160901150427
Keywords
Epigenetic; histone deacetylase inhibitors; chidamide; hematologic and solid cancers; preclinical and clinical trials
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Funding
- Young Scholars Program of Shandong University (YSPSDU) [2016WLJH33]
- Major Project of Science and Technology of Shandong Province [2015ZDJS04001]
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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.
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