摘要
DNA甲基化作为一种重要的表观遗传修饰方式,参与调控多种疾病的发生与发展。蛋白精氨酸甲基转移酶5(protein arginine methyltransferases 5,PRMT5)是真核细胞常见的一种催化组蛋白或非组蛋白甲基化修饰的酶,在多种人类恶性肿瘤中均表达上调,研发PRMT5抑制剂可能成为治疗癌症的一个重要途径。本文针对PRMT5的结构特征、肿瘤相关性以及目前报道的抑制剂进行综述,为PRMT5抑制剂的进一步优化奠定基础。
As an important style of epigenetic modification,DNA methylation participate in the occurrence and development of various disease.Protein arginine methyltransferases 5(PRMT5)was a common enzyme catalyzing the methylation of histone and non-histone protein.It has been found to be upregulated in human malignant tumor,indicating the significance of develop PRMT5 inhibitors.We reviewed the structural features and its relationship with tumor of PRMT5,as well as the reported PRMT5 inhibitors,supporting the further optimization of PRMT5 inhibitors.
作者
黄美玲
肖晶晶
延常姣
凌瑞
Huang Meiling;Xiao Jingjing;Yan Changjiao;Ling Rui(Department of Thyroid,Breast and Vascular Surgery,Xijing Hospital,Air Force Medical University,Shaanxi Xi'an 710032,China)
出处
《现代肿瘤医学》
CAS
2019年第8期1432-1435,共4页
Journal of Modern Oncology
基金
国家自然科学基金(编号:81572917)
关键词
蛋白质精氨酸甲基转移酶
抑制剂
研究进展
protein arginine methyltransferase 5
inhibitors
research progress
