STRUCTURAL INVESTIGATION OF GLYCOSYLTRANSFERASES

这个子项目是许多研究子项目中的一个 由NIH/NCRR资助的中心赠款提供的资源。子项目和 研究者（PI）可能从另一个NIH来源获得了主要资金， 因此可以在其他CRISP条目中表示。所列机构为 研究中心，而研究中心不一定是研究者的研究机构。 我们有兴趣了解几种细菌和人类糖基转移酶的生物学功能和机制。我们已经开发了表达，纯化和动力学特性的糖基转移酶，是重要的细菌发病机制和人类疾病的方法。我们还进行了筛选，以寻找其中一些糖基转移酶的抑制剂。这些抑制剂可以作为这些酶的生物探针，并可以帮助确定这些蛋白质是否是可行的治疗靶点。这项奋进的一个重要方面是获得有关这些目标的结构信息。这些糖基转移酶的结构将是非常宝贵的，为目的的机制的理解和抑制剂的发展。因此，我们感兴趣的是获得这些酶的载脂蛋白形式的结构，与底物结合，并与抑制剂结合。

This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. The subproject and investigator (PI) may have received primary funding from another NIH source, and thus could be represented in other CRISP entries. The institution listed is for the Center, which is not necessarily the institution for the investigator. We are interested in understanding the biological function and mechanism of several bacterial and human glycosyltransferases. We have developed methods to express, purify, and kinetically characterize glycosyltransferases that are important for bacterial pathogenesis and human disease. We have also implemented screens to look for inhibitors of some of these glycosyltranferases. These inhibitors can serve as biological probes of these enzymes and could help determine whether these proteins are viable therapeutic targets. An important aspect of this endeavor is to obtain structural information about these targets. A structure for these glycosyltranferases would be invaluable for the purposes of both mechanistic understanding and inhibitor development. We are therefore interested in obtaining structures of these enzymes in the apo form, with substrate bound, and with inhibitors bound.