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qHTS to Identify Differentiators of Brown Adipocytes

qHTS to Identify Differentiators of Brown Adipocytes
qHTS 鉴定棕色脂肪细胞的分化因子
批准号：
10004996
负责人：
Matthew Hall
金额：
$13.27万
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/10004996
关键词：
AdipocytesAdipose tissueBiological AssayBlood GlucoseBrown FatCardiovascular DiseasesCell Differentiation processCholesterolDevelopmentDiabetes MellitusDyslipidemiasEnergy MetabolismEpidemicFatty acid glycerol estersFutureHumanInformaticsNon-Insulin-Dependent Diabetes MellitusObesityPECAM1 genePatientsPharmaceutical ChemistryPlayRoleWeightdesignhigh throughput screeningimprovedlead optimizationnovelprecursor cellsmall molecule libraries

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中文摘要
翻译
该项目旨在发现具有增加棕色脂肪水平和潜在改善患者体重、胆固醇和糖尿病的能力的新化合物。 在此期间，合作团队利用之前开发的荧光分析(旨在量化人CD31棕色脂肪细胞前体细胞分化)完成了对许多NCGC小分子文库的定量高通量筛选。对HIT分子进行鉴定、螯合和重新测试，以确认其效力并进一步扩大其活性。未来的努力将利用NCGC在药物化学和信息学方面的专业知识来指导Hit-to-Lead优化，以提高最有希望的Hit分子的活性。
英文摘要
This project aims to uncover novel compounds with the capacity to increase brown adipose levels and potentially improve weight, cholesterol, and diabetes in patients. During this period, the collaborative team utilized a previously developed fluorescent assay (designed to quantify human CD31- brown adipocyte precursor cell differentiation) to complete quantitative high-throughput screening of a number of NCGC small molecule libraries. Hit molecules were identified, cherrypicked and retested to confirm potency and further expand on their activity. Future efforts will leverage NCGC expertise in medicinal chemistry and informatics to guide hit-to-lead optimization to improve activity of the most promising hit molecules.
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