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Identification of ALPK1 inhibitors

Identification of ALPK1 inhibitors
ALPK1 抑制剂的鉴定
批准号：
10919704
负责人：
Alexey Zakharov
金额：
$10.0万
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/10919704
关键词：
BiochemicalBiological AssayBlindnessCell LineDiseaseFeverGoalsGoutHeadacheHelicobacter pyloriImmuneInflammationInflammatory Bowel DiseasesInheritedInhibition of NF-KB activationLeadLigandsLinkMalignant NeoplasmsMutationNF-kappa BPeriodicalsPhosphorylationPhosphotransferasesReporterReportingRoleSignal TransductionTNF geneautoinflammatory diseaseshigh throughput screeninginhibitorreduce symptomssensorsmall moleculesmall molecule libraries

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中文摘要
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英文摘要
The goal of the project during the reporting period has been to establish a high-throughput screening assay to assess phosphorylation by ALPK1 upon stimulation by its ligand ADP-heptose. 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. The assay is being screened against small molecule libraries and potential hits have been identified. A biochemical assay will be developed to confirm on target activity.
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