Identification of small molecule RXFP3 ligands

小分子 RXFP3 配体的鉴定

• 批准号: 10688950
• 负责人: Juan Marugan
• 金额: $ 14.62万
• 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/10688950
• 关键词: Addictive Behavior; Agonist; Animal Model; Anorexia Nervosa; Anxiety; Behavioral; Binge Eating; Brain Stem; Cell Culture System; Cell Nucleus; Cells; Cognition; Cyclic AMP; Eating; Eating Disorders; Family; In Vitro; Insulin; Investigation; Ligands; Mental Depression; Neurons; Obesity; Pain; Peptides; Prosencephalon; Receptor Signaling; Relaxin; Stress; Testing; addiction; antagonist; cognitive function; counterscreen; high throughput screening; in vivo; novel; pain processing; receptor; receptor binding; relaxin receptor; response; screening; small molecule; tool; treatment of anxiety disorders; virtual screening

Novel small molecule RXFP3 agonists and antagonists will be valuable tools to elucidate the functions of relaxin-3 and its actions at RXFP3 receptors. During this period, the project team successfully developed a 1536-well high-throughput assay to screen for small molecules that agonize or antagonize the RXFP3 receptor. More than 50,000 small molecules were screened for effects on cAMP levels, and several counterscreens have been developed to characterize screening hits and help identify on-target RXFP3 modulators. Virtual screening was also performed to prioritize candidates for testing.

新型小分子 RXFP3 激动剂和拮抗剂将成为阐明relaxin-3 功能及其对 RXFP3 受体作用的有价值的工具。在此期间，项目团队成功开发了1536孔高通量检测方法，用于筛选激动或拮抗RXFP3受体的小分子。筛选了 50,000 多种小分子对 cAMP 水平的影响，并开发了几种反筛选方法来表征筛选命中并帮助识别目标 RXFP3 调节剂。 还进行了虚拟筛选，以确定测试候选人的优先顺序。