ML199: Inhibitor of Ape1 as a Lead for Cancer Therapeutics

ML199：Ape1 抑制剂作为癌症治疗的先导药物

• 批准号: 9205756
• 负责人: David Maloney
• 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/9205756
• 关键词: ML199; Inhibitor; Ape1; Lead; Cancer

Project highlights: HTS screening and medicinal chemistry optimization lead to a first in class drug like small molecule inhibitor of APE1. The probe molecule ML199 has been delivered to multiple collaborators to study in cancer therapy. Currently pursuing a large screen to identify potent compounds with improved PK properties. 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：HTS 筛选和药物化学优化产生了同类首创药物，如 APE1 小分子抑制剂。探针分子 ML199 已交付给多个合作者，用于癌症治疗研究。目前正在寻求大屏幕来鉴定具有改善 PK 特性的有效化合物。 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。