STRUCTURE BASED DISCOVERY OF ANTIPARASITIC DRUGS AGAINST TRYPANASOMA CRUZI

该提案允许从晶体收集数据， 几种不同的抑制剂与T. cruzi HGPRTase. 铅 已经使用细菌互补来鉴定化合物 筛选方案是由美国大学的合作者开发的。NC在Chapel 之丘 七种化合物已被确定为具有较高的 T. cruzi HPRT酶的活性 HPRTase。 在迄今发现的这七种化合物中， 在结晶实验中进行了测试，并产生了 晶体类型#1 目前正在努力确定抗寄生虫药 药物无疑将受益于拥有最高分辨率的数据， 可能 由于一些抑制剂只允许小的 晶体，同步加速器源是必不可少的长期目标 of this project项目.

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.