Identification of ALPK1 inhibitors
Identification of ALPK1 inhibitors
批准号:
10691144
负责人:
Alexey Zakharov
金额:
$9.0万
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:
Biological AssayBlindnessCell LineDiseaseFeverGoalsGoutHeadacheHelicobacter pyloriHeptosesImmuneInflammationInflammatory Bowel DiseasesInheritedLeadLigandsLinkMalignant NeoplasmsMutationNF-kappa BPathway interactionsPeriodicityPhosphorylationPhosphotransferasesReporterRoleSignal TransductionTNF geneTimeautoinflammatoryhigh throughput screeninginhibitorreduce symptomssensorsmall molecule
中文摘要
本财政年度的项目目标是建立一种高通量筛选(HTS)方法,以评估ALPK1在其配体adp -庚糖刺激下的磷酸化作用。具体来说,该试验利用市售的表达ALPK1的HEK293 NF-kB报告细胞系。候选化合物将在adp -庚糖存在或不存在的情况下评估报告基因激活。随后将评估化合物在tnf - α存在下的“靶标”活性,tnf - α独立于ALPK1激活NF-kB报告基因。此外,将利用表达相同报告基因的ALPK1 KO细胞系来确认化合物对通路的活性。该试验正在优化化合物和配体孵育时间,以及其他参数。
英文摘要
The goal of the project during this fiscal year has been to establish a high-throughput screening (HTS) assay to assess phosphorylation by ALPK1 upon stimulation by its ligand ADP-heptose. Specifically, the assay utilizes a commercially available HEK293 NF-kB reporter cell line expressing ALPK1. Candidate compounds will be evaluated for reporter activation in the presence or absence of ADP-heptose. Compounds will be subsequently evaluated for "on target" activity in the presence of TNF-alpha, which activates the NF-kB reporter independently of ALPK1. Furthermore, ALPK1 KO cell lines expressing the same reporter, will be utilized to confirm compound on pathway activity. The assay is being optimized for compound and ligand incubation time, among other parameters.
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批准号:10691136
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项目类别:
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资助金额:$14.62万
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负责人:Alexey Zakharov
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依托单位:
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批准号:10691135
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资助金额:$14.62万
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负责人:Alexey Zakharov
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批准号:10919702
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资助金额:$24.08万
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资助金额:$10.0万
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批准号:10691142
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资助金额:$25.96万
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资助金额:$12.58万
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依托单位:
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批准号:10691131
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资助金额:$14.62万
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财政年份:--
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依托单位:
Transmission blocking inhibitors of Malaria
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资助金额:$14.62万
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财政年份:--
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依托单位:
Antifungal Antagonism Screening
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批准号:10919697
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项目类别:
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资助金额:$24.08万
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财政年份:--
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负责人:Alexey Zakharov
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依托单位:
Naeglearia fowleri proline tRNA synthetase inhibitors
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批准号:10691134
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项目类别:
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资助金额:$14.62万
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依托单位:
Identification of Myc translation inhibitors
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批准号:10919694
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项目类别:
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资助金额:$24.08万
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财政年份:--
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负责人:Alexey Zakharov
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依托单位:
Antifungal Antagonism Screening
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批准号:10691132
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项目类别:
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资助金额:$25.96万
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财政年份:--
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负责人:Alexey Zakharov
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依托单位:
Identification of Myc translation inhibitors
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批准号:10691129
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项目类别:
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资助金额:$25.96万
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财政年份:--
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负责人:Alexey Zakharov
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依托单位:
海外基金