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High-throughput screening to identify inhibitors of breast-to-brain metastasis

High-throughput screening to identify inhibitors of breast-to-brain metastasis
高通量筛选以确定乳腺至脑转移的抑制剂
批准号：
10916047
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/10916047
关键词：
Automobile DrivingBasic ScienceBiological AssayBrainBreastBreast Epithelial CellsCellsDrug KineticsHealthHumanHuman GenomeMetastatic malignant neoplasm to brainNational Center for Advancing Translational SciencesRare DiseasesResearchRouteToxic effectTranslationsbrain celldrug candidateefficacy studyhigh throughput screeningimprovedin vivoinhibitorinterestnovelpharmacologicprogramssmall moleculetool

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中文摘要
翻译
在此期间，合作团队进行了高通量筛选，以确定相对于正常乳腺上皮细胞选择性杀死乳腺至脑转移细胞的小分子。 出现了几种感兴趣的化合物，这些化合物被推进到药代动力学研究，以表征大脑暴露和选择给药途径。 目前正在进行体内疗效研究。此外，该团队开发了一种基质测定法来鉴定对脑转移细胞显示协同毒性的小分子组合。已经进行了几次组合筛选，该团队正在评估推进疗效研究的选择。
英文摘要
During this period, the collaborative team performed high-throughput screening to identify small molecules that selectively kill breast-to-brain metastatic cells relative to normal breast epithelial cells. Several compounds of interest emerged, which were advanced to pharmacokinetic studies to characterize brain exposure and select route of administration. In vivo efficacy studies are currently underway. Additionally, the team developed a matrix assay to identify small molecule combinations which display synergistic toxicity against brain-metastatic cells. Several combination screens have been performed and the team is assessing options for advancing to efficacy studies.
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