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中文摘要
翻译
在此期间,NCGC致力于进一步鉴定以前在细胞和动物模型中发现的有效和选择性的15-HLO-1抑制剂(ML094和ML351),以确定它们的结合模式并改进它们的配方。 作为一个中心,NCGC与NIH和校外调查人员建立并保持了130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。
英文摘要
During this period, the NCGC worked to further characterize previously identified potent and selective 15-hLO-1 inhibitors (ML094 and ML351) in cellular and animal models, to identify their binding mode and improve their formulation. 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.
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