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: 10688940
• 负责人: Juan Marugan
• 金额: $ 42.54万
• 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/10688940
• 关键词: Atherosclerosis; Binding; Biological Assay; Biology; Cells; Chronic stress; Collaborations; Communities; Development; Disease; Extramural Activities; General Population; Goals; Informatics; Mental Depression; Modeling; PACAPR-1 protein; Pharmaceutical Chemistry; Pharmaceutical Preparations; Phenotype; Process; Publications; Research; Research Personnel; Resources; Study models; Synthesis Chemistry; Translations; United States National Institutes of Health; Validation; Work; antagonist; assay development; base; drug development; drug discovery; high throughput screening; human disease; improved; lead optimization; molecular modeling; neuroblastoma cell; new technology; novel; novel therapeutics; screening; small molecule; small molecule therapeutics; therapeutic development; tool

During this period, a new cell-based assay to examine PAC1 activity in neuroblastoma cells was explored towards high-throughput screening. Molecular modeling studies were performed to identify candidates that bind to PAC1R. The Early Translation Branch (ETB) has 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 ETB 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，人们探索了一种新的基于细胞的检测方法来检查神经母细胞瘤细胞中的 PAC1 活性，以进行高通量筛选。进行分子模型研究以确定与 PAC1R 结合的候选者。 早期翻译分部 (ETB) 与 NIH 和校外研究人员保持着 130 多项积极合作，促进了整个人类疾病谱的药物发现工作。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，ETB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。