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

鉴定脂质激酶 PI5P4Ka/ 抑制剂作为潜在的抗癌药物

• 批准号: 9205789
• 负责人: Matthew Boxer
• 金额: $ 11.4万
• 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/9205789
• 关键词: Identification; Inhibitors; Lipid; Kinase; PI5P4Ka

Project highlights: executed the screen and identified chemical series of interest. Performed medicinal chemistry optimization and validation of the compounds in orthogonal assays such as radiolabeled ATP assays. Determined the mechanism of action of the chemical series as ATP-competitive. Determined the effect of the compounds on cell viability in a variety of cancer cell lines. During this period, the NCGC has fostered and maintained over 180 active collaborations with both NIH and extramural investigators, facilitating drug discovery efforts across the entire spectrum of human disease. These efforts have led to over 100 high-throughput screens and nearly 60 medicinal chemistry campaigns, providing our collaborators and the general research community a wealth of publications and promising small molecule leads. In addition, the NCGC has undertaken a number of informatic challenges to make better use of existing drug and disease target information and provide the general public with easily accessible resources, further catalyzing the development of new therapies for human disease.

项目亮点：执行筛选并确定感兴趣的化学系列。 在正交测定（例如放射性标记 ATP 测定）中对化合物进行药物化学优化和验证。确定了该化学系列的作用机制为 ATP 竞争性。 确定了化合物对多种癌细胞系细胞活力的影响。 在此期间，NCGC 与 NIH 和校外研究人员建立并维持了 180 多项积极合作，促进了整个人类疾病范围的药物发现工作。 这些努力已经促成了 100 多个高通量筛选和近 60 个药物化学活动，为我们的合作者和一般研究界提供了丰富的出版物和有前途的小分子先导化合物。 此外，NCGC还承担了多项信息挑战，以更好地利用现有药物和疾病靶点信息，为公众提供易于获取的资源，进一步促进人类疾病新疗法的开发。