PAC1 receptor antagonists as potential treatments for depression and atherosclerosis associated with chronic stress

PAC1 受体拮抗剂作为慢性应激相关抑郁症和动脉粥样硬化的潜在治疗方法

• 批准号: 10003791
• 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/10003791
• 关键词: Atherosclerosis; Biological Assay; Biology; Chemicals; Chronic stress; Collaborations; Communities; Development; Disease; Evaluation; Extramural Activities; Fostering; General Population; Genomics; Goals; Informatics; Mental Depression; Modeling; PACAPR-1 protein; Pharmaceutical Chemistry; Pharmaceutical Preparations; Phenotype; Process; Publications; Research; Research Personnel; Resources; Series; 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; neurite growth; new technology; novel; novel therapeutics; screening; small molecule; small molecule therapeutics; therapeutic development; tool

During this period, the NCGC completed primary screening of the PAC1 assay, and hit validation is currently underway. Selective hits and chemotypes are under evaluation in neurite growth assay with the aim of rank order series for initiating structure activity-relationship optimization studies. 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完成了PAC1检测的初步筛选，目前正在进行HIT验证。在轴突生长实验中，正在对选择性打击和化学类型进行评估，目的是为了启动结构活性关系优化研究的排序序列。 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。