qHTS to Identify Activators and Inhibitors of Wip1
qHTS to Identify Activators and Inhibitors of Wip1
批准号:
10689608
负责人:
Matthew Hall
金额:
$14.62万
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
关键词:
ApoptoticBindingBiological AssayChemicalsClinicalDNA DamageDrug KineticsEnvironmentFamilyFluorescenceHumanLeadMalignant NeoplasmsMass Spectrum AnalysisPPM1D genePowder dose formPrognosisProtein Serine/Threonine PhosphataseProteinsReporterSurface Plasmon ResonanceTP53 geneanticancer treatmentinhibitormembernoveloverexpressionprotein phosphatase 2Cresponsescaffoldscreeningsmall moleculetherapeutic developmenttumor growth
中文摘要
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英文摘要
During this period, the project team ordered and purified commercially available powders of HTS hits that consisted of both inhibitors and activators of WIP1. We identified one activator and two inhibitors, one competitive and one uncompetitive; these confirmed activity in the the RapidFire mass spectrometry screening assay, the fluorescence reporter orthogonal assay, and binding studies by surface plasmon resonance (SPR). These new scaffolds could be candidates for optimization which may lead to inhibitors with better pharmacokinetics and to the first-in-class WIP1 activator.
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