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Identification of Inhibitors of the Lipid Kinase PI5P4Ka/B as Potential Anti-Cancer Agents

Identification of Inhibitors of the Lipid Kinase PI5P4Ka/B as Potential Anti-Cancer Agents
鉴定脂质激酶 PI5P4Ka/B 抑制剂作为潜在的抗癌药物
批准号：
10004993
负责人：
Min Shen
金额：
$25.03万
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/10004993
关键词：
AddressAntineoplastic AgentsCell physiologyCellsDana-Farber Cancer InstituteDiseaseDisease modelEnzymesEvaluationGrowthIn VitroLeadLipidsMalignant NeoplasmsPhosphatidylinositolsPhosphotransferasesPlayResearchRoleSignal TransductionStructureWorkadvanced diseaseanalogbiological adaptation to stresshigh throughput screeningimprovedin vivo Modelinhibitor/antagonistinsulin signalinginterestkinase inhibitormedical schoolsnovelpharmacokinetics and pharmacodynamicspre-clinicalsmall molecule inhibitorstem

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中文摘要
翻译
这个由威尔·康奈尔医学院、哈佛医学院和达纳·法伯癌症研究所和NCATS的团队组成的合作团队旨在通过发现脂蛋白激酶PI5P4Ka/的新型抑制剂作为潜在的抗癌药物适应症，在先前研究的基础上再接再厉。 在此期间，该团队继续从之前完成的高通量筛查工作中获得成功到领先的评估工作。进行了几轮结构活性研究，以提高感兴趣的HITS的效力和有效性，以及解决物理化学风险。在一些体外和体内模型中，顶级类似物已经被用于详细的表征。
英文摘要
This collaborative team - composed of groups from Weill Cornell Medical College, Harvard Medical School and the Dana Farber Cancer Institute and NCATS - aims to build on previous research by uncovering novel inhibitors of the lipid kinase PI5P4Ka/ as potential anti-cancer agents indications. During this period, the team continued hit-to-lead evaluation efforts stemming from previously completed high-throughput screening efforts. Several rounds of structure activity studies were performed to improve potency and efficacy of hits of interest, as well as to address physiochemical liabilities. The top analogs have been advanced for detailed characterization in a number of in vitro and in vivo models.
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