蛋氨酸合成酶抑制剂的研究进展

Progress in the studies on methionine synthase inhibitors

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.