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BioAssay: AID 647364

Activation of VDR in human HT-29 cells assessed as up-regulation of CYP24A1 at 10 uM by RT-PCR analysis relative to control

A structure-activity relationship study focusing on the A-ring of vitamin D3 (VD3) was undertaken to elucidate its role in inhibiting the Hedgehog pathway and in mediating anti-cancer effects. Analogues resulting from simple functional group substitution at 3' position of VD3 were evaluated in a variety of biological assays to determine their ability to selectively inhibit Hh signaling. more ..
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 Tested Compounds
 Tested Compounds
All(7)
 
 
Unspecified(7)
 
 
 Tested Substances
 Tested Substances
All(7)
 
 
Unspecified(7)
 
 
 Related BioAssays
 Related BioAssays
AID: 647364
Data Source: ChEMBL (804812)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2014-08-24

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=Vitamin D3 receptor; Short=VDR; AltName: Full=1,25-dihydroxyvitamin D3 receptor; AltName: Full=Nuclear receptor subfamily 1 group I member 1
Description ..   
Protein Family: The ligand binding domain of vitamin D receptors, a member of the nuclear receptor superfamily
Comment ..   

Gene:VDR     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: Evaluation of vitamin D3 A-ring analogues as Hedgehog pathway inhibitors.

Abstract: A structure-activity relationship study focusing on the A-ring of vitamin D3 (VD3) was undertaken to elucidate its role in inhibiting the Hedgehog pathway and in mediating anti-cancer effects. Analogues resulting from simple functional group substitution at 3' position of VD3 were evaluated in a variety of biological assays to determine their ability to selectively inhibit Hh signaling. Moderately active Hh inhibitors that have insignificant binding affinity for VDR were identified; however, these compounds also activate the traditional VDR pathway, presumably due to metabolites produced in the cultured cells. Thus, further structural modifications to the VD3 scaffold are required to yield potent, selective Hh inhibitors.
(PMID: 22226657)
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Target Type: Target is a single protein chain
Assay Data Source: Scientific Literature
BAO: Assay Format: cell-based format
Assay Cell Type: HT-29
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)
Data Table ( Complete ):     View All Data
Classification
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