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Identification of small molecule RXFP3 ligands

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
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/10688950
关键词：
Addictive BehaviorAgonistAnimal ModelAnorexia NervosaAnxietyBehavioralBinge EatingBrain StemCell Culture SystemCell NucleusCellsCognitionCyclic AMPEatingEating DisordersFamilyIn VitroInsulinInvestigationLigandsMental DepressionNeuronsObesityPainPeptidesProsencephalonReceptor SignalingRelaxinStressTestingaddictionantagonistcognitive functioncounterscreenhigh throughput screeningin vivonovelpain processingreceptorreceptor bindingrelaxin receptorresponsescreeningsmall moleculetooltreatment of anxiety disordersvirtual screening

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中文摘要
翻译
新的小分子RXFP-3激动剂和拮抗剂将是阐明松弛蛋白-3的功能及其在RXFP-3受体上的作用的有价值的工具。在此期间，项目团队成功地开发了一种1536孔的高通量试验来筛选刺激或拮抗RXFP3受体的小分子。超过50,000个小分子被筛选对cAMP水平的影响，已经开发了几个反筛选来表征筛选命中并帮助识别靶标上的RXFP3调节器。还进行了虚拟筛选，以确定测试候选人的优先顺序。
英文摘要
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.
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会议论文
Kinetic High Throughput Screening for Agonists and Inhibitors of the TRPML1 Ion channel
HTS Assay for Identification of Compounds that Reduce PNC Prevalence
Small molecule agonists of the relaxin 1 receptor
Kinetic High Throughput Screening for Agonists and Inhibitors of the TRPML1 Ion channel
国内基金
海外基金
Agonist-GPR119-Gs复合物的结构生物学研究
  • 批准号：
    32000851
  • 项目类别：
    青年科学基金项目
  • 资助金额：
    24.0万元
  • 批准年份：
    2020
  • 负责人：
    乔安娜
  • 依托单位：
    天津大学