组蛋白去乙酰化酶抑制剂恩替诺特  

A histone deacetylase inhibitor:entinostat

作　　者：李鹏坤[1] 肖桂芝[2] 田红[2] 马海英[1] 

机构地区：[1]中国医科大学附属第四医院药学部,辽宁沈阳110032 [2]天津药物研究院医药信息中心,天津300193

出　　处：《现代药物与临床》2015年第3期341-344,共4页Drugs & Clinic

摘　　要：组蛋白去乙酰化酶(HDAC)是一类对染色质结构修饰和基因表达调控起重要作用的蛋白酶。因HDAC具有转录抑制功能,被视为是一类新兴的癌症药物靶点。HDAC过度表达影响包括乳腺癌在内的一些癌症的进程。抑制HDAC的表达或活性能够为治疗癌症提供新策略。恩替诺特是一种口服合成的苯甲酰胺衍生物类HDAC抑制剂,很有潜力成为抗癌药物,特别是乳腺癌治疗药物。多项临床试验研究表明恩替诺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.

关 键 词：恩替诺特 组蛋白去乙酰化酶 乳腺癌 

分 类 号：R979.1[医药卫生—药品]