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组蛋白乙酰化/去乙酰化是调控基因表达的重要方式之一.目前认为组蛋白乙酰化可促进基因表达,而组蛋白去乙酰化可抑制基因表达.组蛋白去乙酰化酶抑制剂通过竞争性抑制组蛋白去乙酰化酶,使组蛋白乙酰化过程增强。促进基因的表达.白血病中许多染色体易位均涉及组蛋白去乙酰化酶或因组蛋白去乙酰化酶的活性异常,引起抑癌基因表达抑制或癌基因激活和过度表达,导致白血病的发生.在淋巴瘤的发病中,许多类型的淋巴瘤有明确的基因突变,可以产生一些新的基因,如bcl-6基因,导致淋巴瘤的发生.组蛋白去乙酰化酶抑制荆(histone deacety-lase inhibitors,HDAIS)是一类抗恶性血液病的化疗新药.体内和体外实验均显示HDAIS可抑制白血病细胞、淋巴瘤细胞增殖,使细胞周期受阻,诱导肿瘤细胞的分化和/或凋亡.组蛋白去乙酰化酶抑制剂在抗恶性血液病中发挥重要的作用.
Histone acetylation / deacetylation is one of the important ways to regulate gene expression.Hypergysteine is currently believed to promote gene expression, while histone deacetylation can inhibit gene expression.Histatin histone deacetylase inhibitors by competition Inhibitory histone deacetylase, the histone acetylation enhanced. Promote gene expression.Leukemia in many chromosomal translocations involving histone deacetylase or histone deacetylase activity abnormalities, causing inhibition of tumor suppressor gene expression or oncogene activation and overexpression, leading to the occurrence of leukemia. In the development of lymphoma, many types of lymphomas have definite mutations that can produce some new genes, such as the bcl-6 gene, resulting in the development of lymphoma. Histone deacety-lase inhibitors, HDAIS) is a new class of chemotherapeutic drugs against malignant hematologic diseases.It has been shown in vitro and in vivo that HDAIS can inhibit the proliferation of leukemia cells and lymphoma cells, block the cell cycle and induce the differentiation and / or apoptosis of tumor cells.Histatin Sirtuin inhibitors play an important role in anti-haematological malignancies.