Discovery of ML324, a JMJD2 Demethylase Epigenetic Modulator as Potential Antiviral

ML324 的发现，一种 JMJD2 去甲基酶表观遗传调节剂作为潜在的抗病毒药物

• 批准号: 9205748
• 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/9205748
• 关键词: Discovery; ML324; JMJD2; Demethylase; Epigenetic

Project highlights: the probe molecule was characterized for in vivo and in vitro ADME properties. Several top actives were profiled for selectivity and delivered to collaborators to characterize in various oncology models. 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：该探针分子的体内和体外ADME特性得到了表征。对几种顶级活性物质进行了选择性分析，并交付给合作者，以在各种肿瘤学模型中进行表征。 在此期间，NCGC与NIH和校外调查人员进行了180多次积极的合作，促进了整个人类疾病范围内的药物发现工作。这些努力已经产生了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社区提供了丰富的出版物和前景光明的小分子线索。此外，NCGC还承担了一些信息学挑战，以更好地利用现有的药物和疾病目标信息，并为公众提供易于获取的资源，进一步催化人类疾病新疗法的开发。