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发表时间：2007-01-01

发表刊物：化学进展

所属单位：生物工程学院

卷号：19

期号：05

页面范围：762-768

ISSN号：1005-281X

摘要：Histone acetyltransferases ( HAT) and histone deacetylases ( HDACs) as the corresponding enzymes regulate the change of histones in two antagonist forms, acetylated or deacetylated. In recent years, inhibition of HDACs has emerged as a potential strategy in human cancer therapy, since these enzymes play a fundamental role in regulating gene expression and chromatin assembly. The histone deacetylases inhibitors ( HDACIs) are potent inducers of growth arrest, differentiation and apoptosis of tumor cells, and have entered clinical trials for both solid and liquid tumors. However, the molecular basis for their anticancer selectivity remains largely unknown. An improved understanding of the structure and action mechanism of HDAC inhibitors will likely accelerate the clinical development and broaden the future scope and utility of HDAC inhibitors for cancer treatment. In this review, we summarize recent advances of the HDACs inhibitors of cyclic peptide in structure, mechanism of action, clinical development.

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