SMN Ubiquitin Ligase

SMN 泛素连接酶

• 批准号: 10006283
• 负责人: Juan Marugan
• 金额: $ 25.03万
• 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/10006283
• 关键词: Biological Assay; Biology; Chemicals; Collaborations; Communities; Data; Development; Disease; Extramural Activities; Fostering; General Population; Genomics; Goals; Informatics; Lead; Modeling; Pharmaceutical Chemistry; Pharmaceutical Preparations; Phenotype; Process; Publications; Research; Research Personnel; Resources; Structure-Activity Relationship; Synthesis Chemistry; United States National Institutes of Health; Validation; Work; assay development; base; drug development; drug discovery; high throughput screening; human disease; improved; lead optimization; new technology; novel; novel therapeutics; screening; small molecule; small molecule therapeutics; therapeutic development; tool; ubiquitin ligase

During this period, the NCGC has conducted a medicinal chemistry campaign to define structure-activity relationships of the lead chemotypes and further improve their potencies. A new secondary assay has also been under active development to provide further detail and needed activity data to support ongoing medicinal chemistry efforts and better drive SAR determination. As a center, the NCGC has fostered and maintained over 130 active collaborations with both NIH and extramural investigators, facilitating drug discovery efforts across the entire spectrum of human disease. These efforts have led to dozens of high-throughput screens and a number of medicinal chemistry campaigns to further improve on screening hits, providing our collaborators and the general research community with publications and a variety of promising small molecule probes and leads. In addition, the NCGC has worked to advance a number of informatic initiatives 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.

在此期间，NCGC 开展了一项药物化学活动，以确定先导化学型的结构-活性关系并进一步提高其效力。 一种新的二级测定也正在积极开发中，以提供更多细节和所需的活动数据，以支持正在进行的药物化学工作并更好地推动 SAR 测定。 作为一个中心，NCGC 与 NIH 和校外研究人员建立并维持了 130 多项积极合作，促进了整个人类疾病范围的药物发现工作。 这些努力导致了数十次高通量筛选和许多药物化学活动，以进一步提高筛选命中率，为我们的合作者和一般研究界提供出版物和各种有前途的小分子探针和先导化合物。 此外，NCGC还致力于推进多项信息化举措，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。