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AMPK synthetic activators

AMPK synthetic activators
AMPK 合成激活剂
批准号：
10255330
负责人：
Mark Henderson
金额：
$11.24万
依托单位：
NATIONAL CENTER FOR ADVANCING TRANSLATIONAL SCIENCES
依托单位国家：
美国
项目类别：
财政年份：
--
资助国家：
美国
项目状态：
未结题
起止时间：
至
来源：
https://reporter.nih.gov/project-details/10255330
关键词：
5&apos-AMP-activated protein kinaseAdenosine MonophosphateAutophagocytosisBiological AssayBiologyCellsCholesterolCollaborationsDiseaseExtramural ActivitiesGoalsHomeostasisInformaticsLysosomal Storage DiseasesMass Spectrum AnalysisMeasurementMetabolismModelingPathway interactionsPharmaceutical ChemistryPhenotypeProcessProtein KinaseResearchResearch PersonnelScientistStressSynthesis ChemistryTranslationsUnited States National Institutes of HealthValidationWorkassay developmentbasedrug developmentdrug discoveryimprovedinterestlead optimizationmethyl-beta-cyclodextrinnew technologynovelresponsescreeningsmall moleculesmall molecule therapeuticstherapeutic developmenttool

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中文摘要
翻译
在此期间，该团队一直在寻找激活5'腺苷单磷酸活化蛋白激酶（AMPK）的小分子。该团队通过药物化学的努力优化了选择的化学型。AMPK激活剂对Niemann Pick C（一种以胆固醇积累为特征的溶酶体贮积病）有兴趣。该项目团队开发了一种基于质谱的新型高通量分析方法，可以直接测量相关细胞中的胆固醇。这组候选AMPK激活剂正在使用质谱分析进行评估。
英文摘要
During this period the team has pursued small molecules to activate 5' adenosine monophosphate-activated protein kinase (AMPK). The team has optimizing selected chemotype via medicinal chemistry efforts. AMPK activators are of interest for Niemann Pick C, a lysosomal storage disease characterized by cholesterol accumulation. The project team has developed a novel high-throughput mass spectrometry-based assay that allows direct measurement of cholesterol in relevant cells. The set of candidate AMPK activators are being assessed using the mass spectrometry assay.
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