組蛋白去乙?；?HDAC)是一類對染色質(zhì)結(jié)構(gòu)修飾和基因表達(dá)調(diào)控起重要作用的蛋白酶。因HDAC具有轉(zhuǎn)錄抑制功能,被視為是一類新興的癌癥藥物靶點(diǎn)。HDAC過度表達(dá)影響包括乳腺癌在內(nèi)的一些癌癥的進(jìn)程。抑制HDAC的表達(dá)或活性能夠?yàn)橹委煱┌Y提供新策略。恩替諾特是一種口服合成的苯甲酰胺衍生物類HDAC抑制劑,很有潛力成為抗癌藥物,特別是乳腺癌治療藥物。多項(xiàng)臨床試驗(yàn)研究表明恩替諾特具有安全性和有效性。

Histone deacetylase (HDAC) are enzymes, which play an important role in the modification of chromatin structure and gene expression and regulation. Because of the transcriptional suppression function, HDAC are seen as a kind of new cancer drug targets. The overexpression of HDAC affects the progress of some cancers including breast cancer. Inhibiting the expression or activities of HDAC can provide a new strategy for cancer therapy. Entinostat is an oral synthetic benzamide derivative HDAC inhibitor, and has the potential to become a cancer drug, particularly the drug for breast cancer. Many clinical studies indicate that entinostat is effective and safe.