克氏锥虫二氢叶酸还原酶的新型抑制剂
Novel inhibitors of Trypanosoma cruzi dihydrofolate reductase.
作者信息
Zuccotto F, Zvelebil M, Brun R, Chowdhury S F, Di Lucrezia R, Leal I, Maes L, Ruiz-Perez L M, Gonzalez Pacanowska D, Gilbert I H
机构信息
Welsh School of Pharmacy, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff CF10 3XF, UK.
出版信息
Eur J Med Chem. 2001 May;36(5):395-405. doi: 10.1016/s0223-5234(01)01235-1.
There is an urgent need for the development of new drugs to treat Chagas' disease, which is caused by the protozoan parasite Trypanosoma cruzi. The enzyme dihydrofolate reductase (DHFR) has been a very successful drug target in a number of diseases and we decided to investigate it as a potential drug target for Chagas' disease. A homology model of the enzyme was used to search the Cambridge Structural Database using the program DOCK 3.5. Compounds were then tested against the enzyme and the whole parasite. Compounds were also screened against the related parasite, Trypanosoma brucei.
迫切需要开发治疗恰加斯病的新药，恰加斯病由原生动物寄生虫克氏锥虫引起。二氢叶酸还原酶（DHFR）在许多疾病中一直是非常成功的药物靶点，我们决定将其作为恰加斯病的潜在药物靶点进行研究。利用DOCK 3.5程序，使用该酶的同源模型搜索剑桥结构数据库。然后针对该酶和整个寄生虫对化合物进行测试。还针对相关寄生虫布氏锥虫对化合物进行了筛选。
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