DEVELOPMENT OF ISOFORM-SELECTIVE INHIBITORS OF NITRIC OXIDE SYNTHASES (NOS)

一氧化氮合酶 (NOS) 异构体选择性抑制剂的开发

• 批准号: 8170171
• 负责人: HUIYING LI
• 金额: $ 1.29万
• 依托单位: STANFORD UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 2010
• 资助国家: 美国
• 起止时间: 2010-05-01 至 2011-02-28
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/8170171
• 关键词: Animal Testing; Biological Assay; Brain Hypoxia; Cerebral Palsy; Complex; Computer Retrieval of Information on Scientific Projects Database; Development; Enzyme Inhibitor Drugs; Enzyme Inhibitors; Funding; Generations; Grant; In Vitro; Institution; Modification; Nitric Oxide Synthase; Protein Isoforms; Research; Research Personnel; Resources; Source; Structure; United States National Institutes of Health; base; design; information gathering; inhibitor/antagonist; pre-clinical

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. Development of isoform selective NOS inhibitors continues to be the central focus of this proposal. Based on structural information gathered during the two previous proposal periods, a new generation of nNOS selective inhibitors were designed de novo (ref. 1). The new compounds were screened through in vitro inhibitory assays. Those shown to have good potency and selectivity were then used for structural studies. The best inhibitors were also found to protect against cerebral palsy induced by brain hypoxia in pre-clinical animal tests (ref.2). The enzyme-inhibitor complex structures are critical for further modification and improvement of new inhibitors. Therefore, we would like to extend the proposal for another two years.

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