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BioAssay: AID 624266

qHTS for Small Molecule Inhibitors of the ERG Ets/DNA interaction: Summary.

The Ets family of proteins is a family of ~30 conserved transcription factors defined by the presence of an ~85 amino acid domain referred to as the Ets domain, which mediates sequence-specific DNA binding to a core DNA element GGAA/T.The Ets family member ERG has been linked to several neoplasms. ERG has been shown to be frequently over-expressed in prostate cancer. Perhaps more strikingly, ERG more ..
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AID: 624266
Data Source: NCGC (ERG000)
BioAssay Type: Summary, Candidate Probes/Leads with Supporting Evidence
Depositor Category: NIH Molecular Libraries Probe Production Network
Deposit Date: 2012-06-05
Target
Related Experiments
AIDNameTypeComment
624246qHTS for Small Molecule Inhibitors of the ERG Ets/DNA interactionConfirmatorydepositor-specified cross reference: qHTS AID
651803qHTS for Small Molecule Inhibitors of the ERG Ets/DNA interaction: TR assay against cherry picksConfirmatorydepositor-specified cross reference
651804qHTS for Small Molecule Inhibitors of the ERG Ets/DNA interaction: HTRF assay against cherry picksConfirmatorydepositor-specified cross reference
Description:
The Ets family of proteins is a family of ~30 conserved transcription factors defined by the presence of an ~85 amino acid domain referred to as the Ets domain, which mediates sequence-specific DNA binding to a core DNA element GGAA/T.The Ets family member ERG has been linked to several neoplasms. ERG has been shown to be frequently over-expressed in prostate cancer. Perhaps more strikingly, ERG and the Ets protein ETV1 have recently been shown to be the targets of chromosomal translocations with TMPRSS2 which are observed in 80% of prostate cancer patient samples. More extensive studies of the effects of over-expression of ERG in prostate cells have recently been carried out and have shown that over-expression of ERG results in increased invasion.

The importance of DNA-binding to the function of these proteins strongly suggests that inhibiting the DNA binding activity of ERG may be a mechanism to treat prostate cancer as well as other cancers where the activity of ERG plays a key role. We will carry out a high throughout screen to identify inhibitors of the interaction between ERG and DNA using a fluorescence polarization (FP) assay with a His-tagged ERG Ets domain and fluorescently-labeled DNA probes to develop small molecule inhibitors of this interaction as probes to test this hypothesis and lay the groundwork for the development of targeted therapies against ERG.

NIH Molecular Libraries Probe Production Network [MLPCN]
NIH Chemical Genomics Center [NCGC]

Grant: NS066464
PI Name: John Bushweller, University of Virgina
Protocol
Please see linked AIDs for detailed protocols.
Comment
This project is on-going and will be updated a later point.
Additional Information
Grant Number: NS066464

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