Aspartic Protease Inhibitors as Novel Antimalarials
天冬氨酸蛋白酶抑制剂作为新型抗疟药
基本信息
- 批准号:8544739
- 负责人:
- 金额:$ 18.64万
- 依托单位:
- 依托单位国家:美国
- 项目类别:
- 财政年份:2013
- 资助国家:美国
- 起止时间:2013-08-15 至 2016-07-31
- 项目状态:已结题
- 来源:
- 关键词:AcademyAddressAffectAffinity LabelsAntimalarialsAreaArtemisininsAspartic EndopeptidasesBasic ScienceBiological AvailabilityBiologyCessation of lifeChemistryChinese PeopleChloroquineClinicalCollaborationsDevelopmentDiseaseDisease ResistanceDrug CompoundingDrug DesignDrug KineticsDrug TargetingDrug resistanceDrug usageEndoplasmic ReticulumErythrocytesHalf-LifeHealthHumanInstitutesInternationalMalariaMedicineModelingMusOralOutcomeParasite resistanceParasitesPharmaceutical ChemistryPharmaceutical PreparationsPlasmodiumPlasmodium falciparumProcessPropertyProtease InhibitorProteinsResearchResourcesSaintsScienceScientistSolutionsStagingStructureTranslationsUniversitiesVacuoleWorld Healthaffinity labelingartemisininebasecombatcrosslinkdrug discoveryin vivoinhibitor/antagonistkillingsnovelplasmepsinpublic health relevanceresistant straintool
项目摘要
DESCRIPTION (provided by applicant): Malaria is a devastating disease that affects over one billion people and causes approximately 1 million deaths annually. Although there are a number of drugs used to treat the disease, resistance to these drugs is becoming more widespread. Superior long-term solutions for combatting resistant parasites require identification of novel antimalarial drug targets and compound classes that kill the parasite with unique mechanisms of action. Plasmodium falciparum, the most deadly species to humans, as well as other malaria- causing species of Plasmodium, have multiple aspartic proteases that are essential to the parasite's survival. We propose to (1) optimize the antimalarial activity of two classes of asparti protease inhibitors and (2) determine their unique mechanism of action as antimalarial agents. Through our preliminary collaborative efforts, we have already identified drug-like aspartic protease inhibitors with inherent antimalarial activity and oral efficacy for suitable optimizationas drugs. In order to efficiently address the critical need for novel antimalarials, the Center for World Health & Medicine (CWHM) at Saint Louis University has established a research collaboration with the Guangzhou Institutes of Biomedicine and Health (GIBH), Chinese Academy of Sciences. CWHM is a non-profit institute comprised of highly skilled and successful former Pfizer drug discovery scientists with expertise in the translation of basic science into the
discovery and development of novel drugs for challenging targets. GIBH is a leading Chinese center of expertise in malaria biology, drug discovery and medicinal chemistry. This unique collaboration encompasses the expertise and resources necessary to successfully demonstrate the viability of novel aspartic protease inhibitors as antimalarial agents and to determine of thei mechanism(s) of action for target-based drug discovery.
描述(由申请人提供):疟疾是一种毁灭性的疾病,影响超过10亿人,每年造成约100万人死亡。虽然有许多药物用于治疗这种疾病,但对这些药物的耐药性越来越普遍。对抗耐药寄生虫的上级长期解决方案需要确定新的抗疟药物靶标和具有独特作用机制的杀死寄生虫的化合物类别。恶性疟原虫是对人类最致命的物种,以及其他引起疟疾的疟原虫物种,具有多种对寄生虫生存至关重要的天冬氨酸蛋白酶。我们建议:(1)优化两类抗疟蛋白酶抑制剂的抗疟活性;(2)确定它们作为抗疟剂的独特作用机制。通过我们的初步合作努力,我们已经确定了药物样天冬氨酸蛋白酶抑制剂,具有固有的抗疟活性和口服疗效,适合优化为药物。为了有效地解决对新型抗疟药物的迫切需求,圣刘易斯大学世界卫生与医学中心(CWHM)与中国科学院广州生物医药与健康研究院(GIBH)建立了研究合作。CWHM是一个非营利机构,由高技能和成功的前辉瑞药物发现科学家组成,他们在将基础科学转化为
发现和开发具有挑战性的靶点的新药。GIBH是中国领先的疟疾生物学、药物发现和药物化学专业中心。这种独特的合作包括成功证明新型天冬氨酸蛋白酶抑制剂作为抗疟药的可行性以及确定其作用机制以进行靶向药物发现所需的专业知识和资源。
项目成果
期刊论文数量(0)
专著数量(0)
科研奖励数量(0)
会议论文数量(0)
专利数量(1)
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Marvin J Meyers其他文献
Marvin J Meyers的其他文献
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{{ truncateString('Marvin J Meyers', 18)}}的其他基金
Lead optimization of Hepatitis B Virus ribonuclease H inhibitors
乙型肝炎病毒核糖核酸酶 H 抑制剂的先导化合物优化
- 批准号:
10117606 - 财政年份:2020
- 资助金额:
$ 18.64万 - 项目类别:
Lead optimization of Hepatitis B Virus ribonuclease H inhibitors
乙型肝炎病毒核糖核酸酶 H 抑制剂的先导化合物优化
- 批准号:
10308690 - 财政年份:2020
- 资助金额:
$ 18.64万 - 项目类别:
Lead optimization of Hepatitis B Virus ribonuclease H inhibitors
乙型肝炎病毒核糖核酸酶 H 抑制剂的先导化合物优化
- 批准号:
10528443 - 财政年份:2020
- 资助金额:
$ 18.64万 - 项目类别:
Defining approaches for improving HID and HPD compounds as HBV RNaseH antagonists
确定改进 HID 和 HPD 化合物作为 HBV RNaseH 拮抗剂的方法
- 批准号:
9262388 - 财政年份:2017
- 资助金额:
$ 18.64万 - 项目类别:
Aspartic Protease Inhibitors as Novel Antimalarials
天冬氨酸蛋白酶抑制剂作为新型抗疟药
- 批准号:
8721847 - 财政年份:2013
- 资助金额:
$ 18.64万 - 项目类别:
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