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Screening to identify potent and specific inhibitors of N-terminal methyltransferase (NTMT1) as chemical probes

Screening to identify potent and specific inhibitors of N-terminal methyltransferase (NTMT1) as chemical probes
筛选以鉴定有效且特异性的 N 末端甲基转移酶 (NTMT1) 抑制剂作为化学探针
批准号：
10011397
负责人：
Anton Simeonov
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/10011397
关键词：
Biological AssayCardiovascular DiseasesChemicalsCollaborationsCollectionDataDevelopmentDiseaseEpigenetic ProcessFamilyGoalsHistone-Lysine N-MethyltransferaseHistonesInflammationMalignant NeoplasmsMetabolic DiseasesMethylationMethyltransferaseN-terminalNeurodegenerative DisordersProcessProtein MethylationProtein MethyltransferasesProtein-Arginine N-MethyltransferaseProteinsTestingValidationcellular targetingfollow-uphigh throughput screeninginhibitor/antagonistminiaturizescreeningsmall molecule

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中文摘要
翻译
这项合作的目标是发现有效和特定的NTMT1抑制剂作为化学探针，以研究其机制、细胞靶点和功能。 在此期间，合作团队利用先前优化和微型化的NTMT1检测方法对NCGC的几个小分子样品进行了定量高通量筛选。确定的点击是樱桃挑选的初步验证使用初步测试，并随后在后续测试中测试，以提供额外的活性数据。
英文摘要
The goal of this collaboration is to uncover potent and specific inhibitors for NTMT1 as a chemical probe to investigate its mechanism, cellular targets, and functions. During this period, the collaborative team utilized the previously optimized and miniaturized NTMT1 assay to conduct a quantitative high-throughput screen of several of NCGC's small molecule collections. Identified hits were cherry-picked for initial validation using the primary assay, and were subsequently tested in follow-up assays to provide additional activity data.
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