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Identification of small molecule inhibitors of USP8

Identification of small molecule inhibitors of USP8
USP8小分子抑制剂的鉴定
批准号：
10011437
负责人：
Anton Simeonov
金额：
$4.76万
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/10011437
关键词：
Basic ScienceBiological AssayCardiovascular systemCentral obesityCharacteristicsChemicalsChronicCorticotropinDeubiquitinating EnzymeEpidermal Growth Factor ReceptorFutureGlucocorticoidsGoalsImpairmentInfectionLeadLeftMalignant NeoplasmsMutationMyopathyPatientsPharmaceutical ChemistryPhenotypePituitary Gland AdenomaPituitary-dependent Cushing&aposs diseaseProductionResearchSignal TransductionSkinTherapeuticUSP8 geneValidationWeight GainWorkadenomahigh throughput screeningimprovedinhibitor/antagonistknock-downprogramsreproductive functionsmall moleculesmall molecule inhibitorsmall molecule libraries

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中文摘要
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英文摘要
The long term goal of this proposed research program is to develop small molecule chemical probes to inhibit USP8 for basic research and therapeutic purposes. During this period, the collaborative team worked to optimize and implement automated quantitative high-throughput screening (qHTS) of several small molecule libraries. In addition, orthogonal assays were identified and developed to enable further validation of potential USP8 inhibitors identified in the primary screen. Future work will focus on pursuing medicinal chemistry optimization of select hit molecules to further improve their potency, selectivity and other characteristics.
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