蛋氨酸合成酶抑制剂的研究进展  

Progress in the studies on methionine synthase inhibitors

作　　者：王锰[1] 仰佳佳 薛良敏 李灏 刘俊义[1,2] 张志丽[1] 

机构地区：[1]北京大学药学院化学生物学系,北京100191 [2]北京大学天然药物及仿生药物国家重点实验室,北京100191

出　　处：《中国药物化学杂志》2017年第6期466-476,共11页Chinese Journal of Medicinal Chemistry

基　　金：国家自然科学基金项目(21172014);国家自然科学青年基金项目(21302007)

摘　　要：在过去的70年里,叶酸拮抗剂对恶性肿瘤、微生物和寄生虫的感染、慢性炎症等疾病的治疗起到了举足轻重的作用。具有更好性质和活性的新型叶酸拮抗剂的发现仍然吸引着学术界和工业界的广泛关注。蛋氨酸合成酶作为叶酸代谢的关键酶,其对维持人体内的叶酸平衡具有重要作用。如果蛋氨酸合成酶的活性受到抑制,就会从源头阻断叶酸循环杀死细胞。因此蛋氨酸合成酶可以作为潜在的抗肿瘤药物的靶点。本文对蛋氨酸合成酶抑制剂的研究进行综述。For more than 70 years,it has been recognized that antifolates play a key role in treatment of ma- lignant, microbial, parasitic and chronic inflammatory diseases. The discovery of new types of antifolates with improved properties and superior activities still remains an attractive strategy both in academia and in the pharmaceutical industry. Cobalamin-dependent methionine synthase is the pivotal enzyme in the human cells, which plays an important role in maintaining balance of folates. Inhibition of this enzyme can lead to kill cancer cells by blocking folate cycle. So cobalamin-dependent methionine synthase is an excellent target for anticancer drug research. This review mainly presents the development of methionine synthase inhibitors.

关 键 词：蛋氨酸合成酶 钴胺素 蛋氨酸合成酶抑制剂 抗肿瘤 

分 类 号：R979.1[医药卫生—药品]