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BioAssay: AID 502908

Induction of annexin 2-mediated F-actin disruption in human WI38 cells at 4 uM after 2 hrs by confocal laser scanning microscopy

The actin cytoskeleton supports diverse cellular processes such as endocytosis, oriented growth, adhesion and migration. The dynamic nature of the cytoskeleton, however, has made it difficult to define the roles of the many accessory molecules that modulate actin organization, especially the multifunctional adapter protein annexin II. We now report that the compound withaferin A (1) can alter more ..
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Active(1)
 
 
 Tested Substances
 Tested Substances
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Active(1)
 
 
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AID: 502908
Data Source: ChEMBL (652948)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2011-02-25
Modify Date: 2013-11-16

Data Table ( Complete ):           Active    All
Target
Sequence: RecName: Full=Annexin A2; AltName: Full=Annexin II; AltName: Full=Annexin-2; AltName: Full=Calpactin I heavy chain; AltName: Full=Calpactin-1 heavy chain; AltName: Full=Chromobindin-8; AltName: Full=Lipocortin II; AltName: Full=Placental anticoagulant protein IV; Short=PAP-IV; AltName: Full=Protein I; AltName: Full=p36
Description ..   
Protein Family: Annexin
Comment ..   

Gene:ANXA2     Related Protein 3D Structures     More BioActivity Data..
BioActive Compound: 1
Description:
Title: Actin microfilament aggregation induced by withaferin A is mediated by annexin II.

Abstract: The actin cytoskeleton supports diverse cellular processes such as endocytosis, oriented growth, adhesion and migration. The dynamic nature of the cytoskeleton, however, has made it difficult to define the roles of the many accessory molecules that modulate actin organization, especially the multifunctional adapter protein annexin II. We now report that the compound withaferin A (1) can alter cytoskeletal architecture in a previously unknown manner by covalently binding annexin II and stimulating its basal F-actin cross-linking activity. Drug-mediated disruption of F-actin organization is dependent on annexin II expression by cells and markedly limits their migratory and invasive capabilities at subcytotoxic concentrations. Given the extensive ethnobotanical history of withaferin-containing plant preparations in the treatment of cancer and inflammatory and neurological disorders, we suggest that annexin II represents a feasible, previously unexploited target for therapeutic intervention by small-molecule drugs.
(PMID: 16408090)
Categorized Comment
ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 104115

ChEMBL Target Type: Target is a single protein chain

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Activity activity commentActivity activity commentString
2Activity standard flagActivity standard flagInteger
3Activity qualifierActivity qualifierString
4Activity published valueActivity published valueFloat
5Activity standard valueActivity standard valueFloat

Data Table (Concise)
Classification
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