KENDALL NETTLES PRT TIME

肯德尔·荨麻 PRT 时间

• 批准号: 8362134
• 负责人: Kendall W Nettles
• 金额: $ 0.22万
• 依托单位: STANFORD UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 2011
• 资助国家: 美国
• 起止时间: 2011-03-01 至 2012-02-29
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/8362134
• 关键词: Agonist; Binding; Crystallography; Diabetes Mellitus; Drug Design; Estrogen Receptor alpha; Funding; Goals; Grant; Hormones; Ligand Binding Domain; Ligands; Liver diseases; Malignant Neoplasms; National Center for Research Resources; Nuclear; Nuclear Hormone Receptors; Obesity; PPAR gamma; Peroxisome Proliferator-Activated Receptors; Principal Investigator; Protein Family; Proteins; Radiation; Research; Research Infrastructure; Resources; Source; Structure; United States National Institutes of Health; Work; base; cost; human disease; receptor; structural biology; transcription factor

This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. Primary support for the subproject and the subproject's principal investigator may have been provided by other sources, including other NIH sources. The Total Cost listed for the subproject likely represents the estimated amount of Center infrastructure utilized by the subproject, not direct funding provided by the NCRR grant to the subproject or subproject staff. The research focuses on the nuclear hormone family of proteins. Nuclear hormone receptor proteins are ligand inducible transcription factors. Nuclear hormone receptors are involved in several human diseases including cancer, liver disease, obesity, and diabetes. Specifically, we are working with the ligand binding domains of estrogen receptor alpha (ERalpha LBD) and peroxisome proliferator activated receptor gamma (PPAR-gamma). Our goal is to acquire a better understanding of the partial agonism mechanism of these proteins in order to carry out structure based drug design. Experimentally, we desire to characterize several partial agonists bound to PPAR and ER, solve the structures by x-ray crystallography, dissect the atomic level interactions of the ligands, and compare and contrast these interactions and induced allostery with full agonists and antagonists.

该子项目是利用资源的众多研究子项目之一 由 NIH/NCRR 资助的中心拨款提供。子项目的主要支持 并且子项目的主要研究者可能是由其他来源提供的， 包括其他 NIH 来源。 子项目可能列出的总成本 代表子项目使用的中心基础设施的估计数量， NCRR 赠款不直接向子项目或子项目工作人员提供资金。 该研究的重点是蛋白质的核激素家族。 核激素受体蛋白是配体诱导转录因子。 核激素受体与多种人类疾病有关，包括癌症、肝病、肥胖和糖尿病。 具体来说，我们正在研究雌激素受体α（ERα LBD）和过氧化物酶体增殖物激活受体γ（PPAR-γ）的配体结合域。 我们的目标是更好地了解这些蛋白质的部分激动机制，以便进行基于结构的药物设计。 在实验上，我们希望表征与 PPAR 和 ER 结合的几种部分激动剂，通过 X 射线晶体学解析结构，剖析配体的原子水平相互作用，并比较和对比这些相互作用以及与完全激动剂和拮抗剂诱导的变构。