论文部分内容阅读
组蛋白的乙酰化和脱乙酰化在调节基因表达方面起着重要作用,与肿瘤的发生密切相关。具有组蛋乙酰基转移酶(HATs)活性的蛋白均为转录因子活性相关蛋白;组蛋白脱乙酰化酶(HDACs)是转录因子辅助抑制复合物的关键成分。目前发现的HDAC抑制剂结合HDAC催化袋状结构的锌离子,其他部位阻断活性位点的通道而发挥作用;体外培养多种白血病细胞系细胞导致不同程度的分化、凋亡和细胞周期阻滞。体内能抑制荷瘤动物肿瘤生长。
Acetylation and deacetylation of histones play an important role in the regulation of gene expression and are closely related to tumorigenesis. Proteins with histone acetyltransferase (HATs) activity are all transcriptional activity-related proteins. Histone deacetylases (HDACs) are key components of transcription factor-assisted suppression complex. The presently discovered HDAC inhibitors, in combination with HDAC, catalyze the zinc ions in the pouch-like structure, and other sites that block the active site pathways; culturing multiple leukemia cell lines in vitro results in varying degrees of differentiation, apoptosis, and cell cycle arrest . In vivo can inhibit tumor growth in tumor-bearing animals.