组蛋白去乙酰酶抑制剂的药理学研究进展

Advances in pharmacological study of histone deacetylase inhibitors

组蛋白的乙酰化调节,参与了基因表达的调控;组蛋白乙酰转移酶和组蛋白去乙酰酶活性共同决定了组蛋白的乙酰化水平。组蛋白去乙酰酶抑制剂可提高组蛋白的乙酰化水平,并对一些非组蛋白成分产生影响,从而调节某些特定基因的表达。综述了组蛋白去乙酰酶抑制剂的药理作用及其临床应用前景。

Acetylation of histone involves in the regulation of gene expression. The level of his-tone acetylation is determined by the activities of histone acetyltransferases and histone deacetylases. Histone deacetylase inhibitors increase the acetylation level of histone as well as some non-histone proteins , and specifically modulate some gene expression. The pharmacological actions of histone deacetylase inhibitors and their potential clinical uses were reviewed.