NANODISCS: CYTOCHROME P450 DRUG INTERACTIONS

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。列出的机构是 研究中心，而研究中心不一定是研究者所在的机构。 已经开发了脂质膜模拟物（Nanodisc）来研究膜蛋白。 纳米盘已被证明对研究细胞色素P450单加氧酶家族有价值，其中CYP 3A 4在人类肝脏中最丰富。 这个家族的特殊成员代谢了大约50%的商业药物。 我们的目标是研究许多结合CYP 3A 4的药物样底物，同时结合到脂质膜的自然环境中。 我们希望了解利用我们的PLIMSTEX方案结合药物靶标后的结合亲和力、化学计量和局部构象变化。

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. A lipid membrane mimetic (Nanodisc) has been developed to study membrane proteins. Nanodiscs have been demonstrated to be valuable to study the cytochrome P450 monooxygenase family, with CYP3A4 being the most abundant in human liver. This particular member of the family metabolizes approximately 50% of commercial drugs. Our goal is to study many of the drug-like substrates that bind to CYP3A4 while incorporated into the natural environment of the lipid membrane. We wish to learn about binding affinities, stoichiometry, and localized conformational changes upon binding the drug targets utilizing our PLIMSTEX protocols.