CRYSTALLOGRAPHIC STRUCTURE ANALYSES OF PROTEIN/LIGAND COMPLEXES

蛋白质/配体复合物的晶体结构分析

• 批准号: 7721730
• 负责人: Ronald E Stenkamp
• 金额: $ 0.02万
• 依托单位: STANFORD UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 2008
• 资助国家: 美国
• 起止时间: 2008-03-01 至 2009-02-28
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7721730
• 关键词: Complex; Computer Retrieval of Information on Scientific Projects Database; Data Set; Drug Delivery Systems; Drug Design; Enzymes; Funding; G-Protein-Coupled Receptors; Glutathione S-Transferase; Grant; Institution; Ligand Binding; Ligands; Molecular; Pattern; Pharmaceutical Preparations; Property; Proteins; Research; Research Personnel; Resolution; Resources; Rhodopsin; Signal Transduction; Source; Streptavidin; Structure; Time; United States National Institutes of Health; Vision; biotin-binding protein; biotin-streptavidin complex; detoxication; mutant; research study; synchrotron radiation; ultra high resolution

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. Beam time is requested for three crystallographic projects studying protein/ligand interactions. Rhodopsin is the G-protein coupled receptor (GPCR) involved in the first molecular steps in vision. Several specialized experiments for observing the conformational change leading to signal transduction for this protein are planned. These experiments will have considerable impact on drug design efforts for other GPCRs making up about a third of all current drug targets. Beam time will also be used for continued studies of streptavidin mutants to aid in understanding the tight binding of the protein and biotin. Synchrotron radiation is needed to study small crystals and obtain ultra-high resolution data sets for some of the streptavidin/biotin complexes. Finally, beam time is requested for glutathione S-transferase complexes and mutants yielding small crystals or high resolution diffraction patterns. These studies are aimed at understanding the mechanism and ligand binding properties of this drug detoxication enzyme.

该子项目是利用该技术的众多研究子项目之一 资源由 NIH/NCRR 资助的中心拨款提供。子项目和 研究者 (PI) 可能已从 NIH 的另一个来源获得主要资金， 因此可以在其他 CRISP 条目中表示。列出的机构是 对于中心来说，它不一定是研究者的机构。 研究蛋白质/配体相互作用的三个晶体学项目需要束流时间。 视紫质是一种 G 蛋白偶联受体 (GPCR)，参与视觉的第一个分子步骤。 计划进行几项专门实验来观察导致该蛋白质信号转导的构象变化。 这些实验将对其他 GPCR 的药物设计工作产生相当大的影响，这些 GPCR 约占当前所有药物靶点的三分之一。 束流时间还将用于链霉亲和素突变体的继续研究，以帮助了解蛋白质和生物素的紧密结合。 需要同步辐射来研究小晶体并获得一些链霉亲和素/生物素复合物的超高分辨率数据集。 最后，谷胱甘肽 S-转移酶复合物和突变体产生小晶体或高分辨率衍射图案需要光束时间。 这些研究旨在了解这种药物解毒酶的机制和配体结合特性。