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High Throughput Screening for Biased Agonists of the TSH Receptor that Activate the Beta-arrestin pathway

High Throughput Screening for Biased Agonists of the TSH Receptor that Activate the Beta-arrestin pathway
高通量筛选激活 β-抑制蛋白途径的 TSH 受体偏向激动剂
批准号：
10688945
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
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/10688945
关键词：
AgonistArrestin Beta 1BiologyCell LineCollaborationsDiseaseEvaluationExtramural ActivitiesGoalsInformaticsMetabolicModelingOsteoporosisPathway interactionsPharmaceutical ChemistryPhenotypeProcessResearchResearch PersonnelSeriesSignal TransductionSynthesis ChemistryTestingThyrotropin ReceptorTranslationsUnited States National Institutes of HealthValidationWorkanalogassay developmentbasebeta-arrestindrug developmentdrug discoveryfollow-uphigh throughput screeninglead optimizationmouse modelnew technologynoveloverexpressionscreeningsmall moleculesmall molecule therapeuticstherapeutic developmenttool

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中文摘要
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英文摘要
The main goal of this project is to develop a potent and selective small molecule TSHR agonist, with biased signaling profile. During this period, the most promising hits from high-throughput screening were identified and followed up with medicinal chemistry and several series of analogs were synthesized. Candidates with attractive activity profiles were pursued with medicinal chemistry to synthesize a series of new analogs, which were advanced for testing in a TSHR overexpressing cell line to determine beta-Arrestin 1 signaling. Pharamcokinetics of the most potent, selective and metabolically stable molecules were carried out. The optimized lead molecule is under evaluation in efficacy mouse models of osteoporosis.
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