STRUCTURE BASED DISCOVERY OF ANTIPARASITIC DRUGS AGAINST TRYPANASOMA CRUZI

这项提议是允许从水晶中收集数据， 几种不同的抑制剂与克鲁兹毛滴虫HGPRTase结合。铅 化合物已通过细菌互补作用进行了鉴定 由北卡罗来纳大学教堂分校的合作者开发的筛查方案 小山。已确认有七种化合物具有较高的 克氏毛滴虫HPRTase对人体的抑制作用 HPRTase。到目前为止，在这七种化合物中，有四种 已经在结晶实验中进行了测试，并生产了 类型1的晶体。这项正在进行的识别抗寄生虫的努力 药物无疑将受益于拥有最高分辨率的数据 有可能。由于一些抑制剂只允许小鼠生长 晶体，同步加速器源对于长期目标是不可或缺的 这个项目的。

This proposal is to allow data collection from crystals with several different inhibitors bound to the T. cruzi HGPRTase. Lead compounds have been identified using bacterial complementation screening protocol developed by collaborators at U. of NC at Chapel Hill. Seven compounds have been identified as having higher inhibitory effect of the T. cruzi HPRTase than they have on the human HPRTase. Of these seven compounds identified to date, four of them have been tested in crystallizatioon experiments and have produced crystals of type #1. This ongoing effort to identify antiparasitic drugs will undoubtedly benefit from having the highest resolution data possible. Since some of the inhibitors only allow the growth of small crystals, synchrotron sources are indispensible to the long term goal of this project.