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BioAssay: AID 762114

Induction of Nrf2/Keap1 in human HCT116 cells assessed as induction of ARE activity at 50 uM after 12 hrs by luciferase reporter gene assay relative to control

When exposed to electrophiles, human colorectal cancer cells (HCT116) counteract oxidative stress through activating NF-E2-related factor 2 (Nrf2)/antioxidant response element (ARE) pathway. To identify new activators, luciferase reporter gene assay was used to screen in-house database of our laboratory, leading to a novel alpha-pyrone compound 1 as a hit. 2 with 2-fluoro phenyl group exhibited more ..
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 Tested Compounds
 Tested Compounds
All(26)
 
 
Unspecified(26)
 
 
 Tested Substances
 Tested Substances
All(26)
 
 
Unspecified(26)
 
 
 Related BioAssays
 Related BioAssays
AID: 762114
Data Source: ChEMBL (973861)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2014-05-03
Modify Date: 2014-08-24

Data Table ( Complete ):           View All Data
Targets
Sequence: RecName: Full=Nuclear factor erythroid 2-related factor 2; Short=NF-E2-related factor 2; Short=NFE2-related factor 2; AltName: Full=HEBP1; AltName: Full=Nuclear factor, erythroid derived 2, like 2
Description ..   
Protein Family: basic leucine zipper DNA-binding and multimerization region of GCN4 and related proteins
Comment ..   

Gene:NFE2L2     Related Protein 3D Structures     More BioActivity Data..


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Tested Compounds:
Description:
Title: Synthesis and bioevaluation of a series of alpha-pyrone derivatives as potent activators of Nrf2/ARE pathway (part I).

Abstract: When exposed to electrophiles, human colorectal cancer cells (HCT116) counteract oxidative stress through activating NF-E2-related factor 2 (Nrf2)/antioxidant response element (ARE) pathway. To identify new activators, luciferase reporter gene assay was used to screen in-house database of our laboratory, leading to a novel alpha-pyrone compound 1 as a hit. 2 with 2-fluoro phenyl group exhibited the strongest ARE inductive activity in the first round structure-activity relationship (SAR) study. Biological studies showed the compound induced nuclear translocation of Nrf2 preceded by phosphorylation of ERK1/2. The data encouraged us to use 2 as lead and 20 derivatives were synthesized to discuss a more detailed SAR, leading to a more potent compound 9, which can be the starting compound for further modification.
(PMID: 23820128)
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Target Type: PROTEIN-PROTEIN INTERACTION
Assay Data Source: Scientific Literature
BAO: Assay Format: cell-based format
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1FC activity commentFC activity commentString
2FC standard flagFC standard flagInteger
3FC qualifierFC qualifierString
4FC published valueFC published valueFloat
5FC standard valueFC standard valueFloat

Data Table (Concise)
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