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AMPK synthetic activators

AMPK synthetic activators
AMPK 合成激活剂
批准号：
10916050
负责人：
Mark Henderson
金额：
$24.08万
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/10916050
关键词：
5&apos-AMP-activated protein kinaseAdenosine MonophosphateAutophagocytosisBiological AssayCellsCholesterolDataDiseaseHomeostasisLysosomal Storage DiseasesMass Spectrum AnalysisMeasuresMetabolismModelingNational Center for Advancing Translational SciencesPathway interactionsPharmaceutical ChemistryProtein KinaseScientistStressTestingWorkefficacy studyimprovedin vivomethyl-beta-cyclodextrinnovelresponsesmall molecule

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中文摘要
翻译
在此期间，合作团队致力于表征先前发现的激活5'腺苷单磷酸活化蛋白激酶（AMPK）的许多小分子撞击。该团队通过药物化学的努力优化了选择的化学型，并实施了一种新的高通量质谱分析来测量胆固醇，以测试化合物的活性。在Niemann Pick C（一种以胆固醇积累为特征的溶酶体贮积病）的背景下测试了顶部活性。该团队正在利用质谱数据提名少量化合物进行额外的基于细胞的表征，随后进行体内功效研究。
英文摘要
During this period the collaborative team has worked to characterize a number of small molecule hits previously found to activate 5' adenosine monophosphate-activated protein kinase (AMPK). The team has optimized select chemotypes via medicinal chemistry efforts and implemented a novel high-throughput mass spectrometry assay to measure cholesterol to test activity of the compounds. Top actives were tested in the context of Niemann Pick C, a lysosomal storage disease characterized by cholesterol accumulation. The team is utilizing mass spectrometry data to nominate a small number of compounds for additional cell based characterization, followed by in vivo efficacy studies.
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