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STRUCTURE BASED DRUG DESIGN FOR TREATMENT OF PARASITIC AND VIRAL DISEASES

STRUCTURE BASED DRUG DESIGN FOR TREATMENT OF PARASITIC AND VIRAL DISEASES
用于治疗寄生虫和病毒性疾病的基于结构的药物设计
批准号:
8169745
负责人:
James H. McKerrow
金额:
$0.18万
依托单位国家:
美国
项目类别:
财政年份:
2010
资助国家:
美国
项目状态:
已结题
起止时间:
2010-09-12 至 2011-05-31

项目摘要

项目成果

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中文摘要
翻译
这个子项目是许多研究子项目中利用 资源由NIH/NCRR资助的中心拨款提供。子项目和 调查员(PI)可能从NIH的另一个来源获得了主要资金, 并因此可以在其他清晰的条目中表示。列出的机构是 该中心不一定是调查人员的机构。 我们这个项目的目标是设计和合成新的多肽和类似肽的抑制剂,特别针对疟疾、血吸虫病、锥虫病和甲型肝炎发病机制中的关键蛋白酶。晶体结构和在某些情况下基于同源的靶蛋白结构模型被用于基于计算机图形的配基结合的建模、用于潜在抑制剂的数据库筛选以及潜在的结合模式的分析。优化这些化合物的目的是提高特异性、半衰期和降低毒性。利用药物化学方法,我们设计和合成了多种化合物,包括杂芳烃抑制剂、多肽类和模拟多肽类抑制剂。在该项目的最初几年,质谱学在这些先导化合物的化学表征中发挥了重要作用。蛋白质组学分析在靶标鉴定的早期阶段也很重要,使用基于亲和力的探针来靶向特定功能亚类的蛋白酶活性。
英文摘要
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. Our goal for this project is to design and synthesize novel peptide and peptido-mimetic inhibitors, specifically targeted against proteases central to the pathogenesis of malaria, schistosomiasis, trypanosomiasis, and hepatitis A. Crystal structures and in some cases homology-based structural models for target proteases are used for computer-graphics based modeling of ligand binding, for database screening of potential inhibitors as well as for analysis of potential binding modes. Optimization of these compounds is aimed at improving specificity, half-life, and diminishing toxicity. Using medicinal chemistry approaches, we have designed and synthesized a wide variety of chemical compounds which include heteroaromatic inhibitors, peptide-based and peptidomimetic inhibitors. In the early years of this project, mass spectrometry has played an important role in chemical characterization of these lead compounds. Proteomic analysis is also important at early stages of target identification, using affinity based probes that target specific functional subclasses of protease activities.
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会议论文
Evaluation of a cathepsin S inhibitor as a potential drug for Chagas disease
HYDROLYSIS OF HEMOGLOBIN BY SCHISTSOMA MANSONI CATHEPSIN B-LIKE CYSTEINEPROTEASE
STRUCTURE BASED DRUG DESIGN FOR TREATMENT OF PARASITIC AND VIRAL DISEASES
GIARDIA LAMBLIA CYSTEINE PROTEASES: TRAFFICKING, LOCALIZATION, AND FUNCTION
国内基金
海外基金
帽结合蛋白(cap binding protein)调控乙烯信号转导的分子机制
  • 批准号:
    32170319
  • 项目类别:
    面上项目
  • 资助金额:
    58.00万元
  • 批准年份:
    2021
  • 负责人:
    董春海
  • 依托单位:
帽结合蛋白(cap binding protein)调控乙烯信号转导的分子机制
  • 批准号:
    --
  • 项目类别:
    --
  • 资助金额:
    58万元
  • 批准年份:
    2021
  • 负责人:
    董春海
  • 依托单位:
ID1 (Inhibitor of DNA binding 1) 在口蹄疫病毒感染中作用机制的研究
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  • 批准号:
    31372080
  • 项目类别:
    面上项目
  • 资助金额:
    80.0万元
  • 批准年份:
    2013
  • 负责人:
    杨迎伍
  • 依托单位: