Discovery of Inhibitors of Human 5-Lipoxygenase and CYP51 as Anti-Fungal Leads

人类 5-脂氧合酶和 CYP51 抑制剂作为抗真菌先导化合物的发现

• 批准号: 9205750
• 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/9205750
• 关键词: Discovery; Inhibitors; Human; Lipoxygenase; CYP51

Project highlights: completed Medicinal chemistry optimization and tested compounds against 5-hLO and CYP51. A modified version of antifungal agent ketaconazole was synthesized and scaled up. 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：完成药物化学优化并针对 5-hLO 和 CYP51 测试化合物。合成并放大了抗真菌剂酮康唑的改良版本。 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。