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
• 资助国家: 美国
• 起止时间: 至
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/10004993
• 关键词: Address; Antineoplastic Agents; Cell physiology; Cells; Dana-Farber Cancer Institute; Disease; Disease model; Enzymes; Evaluation; Growth; In Vitro; Lead; Lipids; Malignant Neoplasms; Phosphatidylinositols; Phosphotransferases; Play; Research; Role; Signal Transduction; Structure; Work; advanced disease; analog; biological adaptation to stress; high throughput screening; improved; in vivo Model; inhibitor/antagonist; insulin signaling; interest; kinase inhibitor; medical schools; novel; pharmacokinetics and pharmacodynamics; pre-clinical; small molecule inhibitor; stem

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.

这个合作团队-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的小组组成-旨在通过发现脂质激酶PI 5 P4 Ka/的新型抑制剂作为潜在的抗癌药物适应症来建立以前的研究。 在此期间，该团队继续从先前完成的高通量筛选工作中进行命中到领先的评估工作。进行了几轮结构活性研究，以提高目标命中物的效价和有效性，并解决理化问题。已经在许多体外和体内模型中对顶级类似物进行了详细表征。