Identification of Inhibitors of Myosin Polymerization as Novel Therapies for Asthma

鉴定肌球蛋白聚合抑制剂作为哮喘新疗法

• 批准号: 9554479
• 负责人: Anton Simeonov
• 金额: $ 25.16万
• 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/9554479
• 关键词: Alternative Therapies; Asthma; Biology; Cells; Chemicals; Collaborations; Communities; Development; Disease; Extramural Activities; Fostering; General Population; Genomics; Goals; Informatics; Lead; Modeling; Myosin ATPase; Pharmaceutical Chemistry; Pharmaceutical Preparations; Phenotype; Process; Publications; Research; Research Personnel; Resources; Safety; Smooth Muscle Myosins; Synthesis Chemistry; United States National Institutes of Health; Validation; Work; assay development; base; drug development; drug discovery; high throughput screening; human disease; improved; inhibitor/antagonist; interest; new technology; novel; novel therapeutics; polymerization; respiratory smooth muscle; screening; small molecule; small molecule inhibitor; small molecule therapeutics; therapeutic development; tool

During this period, the NCGC has performed extensive screening for small molecules that inhibit smooth muscle myosin polymerization, and have characterized hits of interest in a number of advanced cell-based models. In addition, an extensive medicinal chemistry campaign has been undertaken to further optimize lead compounds for efficacy, potency, safety and selectivity. 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 对抑制平滑肌肌球蛋白聚合的小分子进行了广泛的筛选，并在许多先进的基于细胞的模型中表征了感兴趣的目标。 此外，还开展了广泛的药物化学活动，以进一步优化先导化合物的功效、效力、安全性和选择性。 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。