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

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：
10916021
负责人：
Juan Marugan
金额：
$31.01万
依托单位：
NATIONAL CENTER FOR ADVANCING TRANSLATIONAL SCIENCES
依托单位国家：
美国
项目类别：
财政年份：
--
资助国家：
美国
项目状态：
未结题
起止时间：
至
来源：
https://reporter.nih.gov/project-details/10916021
关键词：
AtherosclerosisBiological AssayBiologyCell LineCellsChronic stressCollaborationsDiseaseExtramural ActivitiesFollow-Up StudiesGoalsInformaticsMental DepressionModelingNeuroblastomaPACAPR-1 proteinPharmaceutical ChemistryPhenotypeProcessReporterResearchResearch PersonnelSynthesis ChemistryTestingTranslationsUnited States National Institutes of HealthValidationWorkantagonistassay developmentdrug developmentdrug discoveryhigh throughput screeninglead optimizationmolecular modelingneuroblastoma cellnew technologynovelscreeningsmall moleculesmall molecule therapeuticstherapeutic developmenttoolvirtual screening

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中文摘要
翻译
在此期间，一种基于细胞的检测神经母细胞瘤细胞中PAC1活性的方法被用于高通量筛选，以测试大约4000种化合物。通过分子建模和虚拟筛选研究选择的另外200个化合物也被测试了拮抗PAC1R的能力。该团队对筛选出的一组最有希望的化合物进行了后续研究。正在考虑利用神经母细胞瘤报告细胞系进行额外的高通量筛查。
英文摘要
During this period, a cell-based assay to examine PAC1 activity in neuroblastoma cells was used for high-throughput screening to test approximately 4000 compounds. An additional 200 compounds selected through molecular modeling and virtual screening studies were also tested for ability to antagonize PAC1R. The team has performed follow up studies on a set of the most promising compounds from screening. Additional high-throughput screening utilizing the neuroblastoma reporter cell line is being considered.
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