qHTS to Identify Inhibitors of Mutant and Wildtype NSD2

qHTS 鉴定突变型和野生型 NSD2 抑制剂

• 批准号: 9359919
• 负责人: Matthew Hall
• 金额: $ 3.75万
• 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/9359919
• 关键词: Biological Assay; Biology; Chemicals; Chromatin; Collaborations; Communities; Development; Disease; EZH2 gene; Extramural Activities; Fostering; Gene Activation; Gene Fusion; General Population; Genomics; Goals; Histone H3; Informatics; Lead; Lysine; Modeling; Multiple Myeloma; Oncogenic; Pharmaceutical Chemistry; Pharmaceutical Preparations; Process; Protein Isoforms; Publications; Recurrence; Research; Research Personnel; Resources; Role; Site; Synthesis Chemistry; United States National Institutes of Health; Validation; WHSC1 gene; Work; assay development; base; drug development; drug discovery; high throughput screening; histone methyltransferase; human disease; improved; inhibitor/antagonist; interest; mutant; new technology; novel therapeutics; overexpression; screening; small molecule; small molecule therapeutics; therapeutic development; tool

During this period, the NCGC has worked to adapt and optimize an HTS-amenable NSD2 assay to enable high-throughput screening. As a center, the NCGC has fostered and maintained over 110 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一直致力于调整和优化符合HTS的NSD2检测方法，以实现高通量筛查。 作为一个中心，NCGC与NIH和校外调查人员建立并保持了110多个积极的合作，促进了人类疾病整个谱系的药物发现工作。这些努力导致了数十个高通量筛选和许多药物化学活动，以进一步改进筛选命中，为我们的合作者和一般研究社区提供出版物和各种有前途的小分子探针和线索。此外，NCGC还致力于推进多项信息学倡议，以更好地利用现有的药物和疾病目标信息，并向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。