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BioAssay: AID 502906

Inhibition of annexin 2-mediated liposome aggregation after 15 mins by spectrophotometry

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(2)
 
 
Active(1)
 
 
Inactive(1)
 
 
 Tested Substances
 Tested Substances
All(2)
 
 
Active(1)
 
 
Inactive(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 502906
Data Source: ChEMBL (652946)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2011-02-25
Modify Date: 2014-05-26

Data Table ( Complete ):           View Active Data    View All 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)
Comment
Putative Target:

ChEMBL Target ID: 104115
Target Type: SINGLE PROTEIN
Pref Name: Annexin A2
Synonyms: Annexin A2;Annexin II;Annexin-2;Calpactin I heavy chain;Calpactin-1 heavy chain;Chromobindin-8;Lipocortin II;p36;PAP-IV;Placental anticoagulant protein IV;Protein I;
Gene Name: ANX2 ;ANX2L4;ANXA2;CAL1H;LPC2D;
Protein Accession: P07355;
Protein GI: 113950;
Organism: Homo sapiens
Tax ID: 9606
Target Classification: ion channel other annexin
Confidence: Homologous single protein target assigned
Relationship Type: Homologous protein target assigned
Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

BAO: Assay Format: biochemical format

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Inhibition activity commentInhibition activity commentString
2Inhibition standard flagInhibition standard flagInteger
3Inhibition qualifierInhibition qualifierString
4Inhibition published valueInhibition published valueFloat
5Inhibition standard valueInhibition standard valueFloat

Data Table (Concise)
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