Identification of Inhibitors of Nrf2 Expression

Nrf2 表达抑制剂的鉴定

• 批准号: 9205794
• 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/9205794
• 关键词: Identification; Inhibitors; Nrf2; Expression

Project highlights: the full compound library was screened and a lead chemotype was identified for development. Medicinal chemistry was undertake to improve activity, and a number of advanced cell-based assays were pursued to characterize cellular and anticancer activity of these compounds. 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：筛选了完整的化合物库并确定了用于开发的先导化学型。 人们进行了药物化学来提高活性，并进行了许多先进的基于细胞的测定来表征这些化合物的细胞和抗癌活性。 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。