REQUEST FOR SUPPORT OF A TEACHING POSTDOCTORAL FELLOW

请求博士后教学人员的支持

• 批准号: 8360110
• 负责人: Stefan Franz Paula
• 金额: $ 6.39万
• 依托单位: UNIVERSITY OF LOUISVILLE
• 依托单位国家: 美国
• 财政年份: 2011
• 资助国家: 美国
• 起止时间: 2011-05-01 至 2012-04-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/8360110
• 关键词: Antineoplastic Agents; Biological Assay; Biomedical Research; Ca(2+)-Transporting ATPase; Computational Technique; Docking; Educational process of instructing; Endoplasmic Reticulum; Enzyme Inhibitor Drugs; Enzyme Inhibitors; Enzymes; Funding; Grant; Hydroquinones; Libraries; Ligands; Modeling; National Center for Research Resources; Physiological Processes; Postdoctoral Fellow; Principal Investigator; Research; Research Infrastructure; Resources; Role; Series; Source; Structure-Activity Relationship; Testing; United States National Institutes of Health; base; cost; hydroquinone; inhibitor/antagonist; novel; tool

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. Inhibitors of the enzyme sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) are valuable research tools for the study of the enzyme's role in physiological processes and they also have the potential of being developed into new anti-cancer agents. A series of 2,5-disubstitued hydroquinones will be synthesized and their ability to inhibit SERCA will be assessed in bioassays. Based on the results, computational techniques such as structure-activity relationship modeling and ligand docking will be used to develop models capable of predicting the activities of yet untested, hydroquinone-based compounds. With the aid of these models, compound libraries will be screened virtually for novel SERCA inhibitors that then will be obtained and tested in bioassays.

这个子项目是许多利用资源的研究子项目之一 由NIH/NCRR资助的中心拨款提供。子项目的主要支持 而子项目的主要调查员可能是由其他来源提供的， 包括其它NIH来源。 列出的子项目总成本可能 代表子项目使用的中心基础设施的估计数量， 而不是由NCRR赠款提供给子项目或子项目工作人员的直接资金。 肌浆网/内质网Ca ~（2+）-ATP酶（SERCA）抑制剂是研究该酶在生理过程中作用的重要工具，也具有开发成为新的抗癌药物的潜力。将合成一系列2，5-二取代对苯二酚，并在生物测定中评估其抑制SERCA的能力。基于这些结果，计算技术，如结构-活性关系建模和配体对接将用于开发能够预测尚未测试的基于氢醌的化合物的活性的模型。借助这些模型，化合物库将被筛选出新的SERCA抑制剂，然后将获得并在生物测定中进行测试。