ETV1

The closely related TFs ERG and ETS variant 1 (ETV1) are frequently found to be involved in protein fusions causing, or playing a crucial role in, prostate cancer[1], among others, where they are often dysregulated by genomic derangement. ETV1 is an ETS factor gene that undergoes chromosomal translocation in prostate cancers and Ewing's sarcomas amplification in melanomas, and lineage dysregulation in gastrointestinal stromal tumors. ETV1 is phosphorylated downstream of mitogen-activated protein kinase (MAPK) signaling, which enhances its protein stability. In addition, the histone acetyltransferase (HAT) p300 binds and acetylates ETV1 at lysine residues, leading to increased protein half-life and enhanced transcriptional activity[2]. ETV1 targets MMP7, MMP13, FKBP10 and GLYATL2 genes, among several others[3].


[1] S. Rahim et al. YK-4-279 inhibits ERG and ETV1 mediated prostate cancer cell invasion. PLoS One. 2011 Apr 29;6(4):e19343.
[2] M.S. Pop et al. A small molecule that binds and inhibits the ETV1 transcription factor oncoprotein. Mol Cancer Ther. 2014 Jun;13(6):1492-502.
[3] S. Rahim et al. A small molecule inhibitor of ETV1, YK-4-279, prevents prostate cancer growth and metastasis in a mouse xenograft model. PLoS One. 2014 Dec 5;9(12):e114260.

1 Item(s)

per page
Axon ID Name Description From price
2469 YK 4-279 Inhibitor of ETV1, ERG and interactions of EWS-FLI1 and RNA helicase A €95.00

1 Item(s)

per page
Please wait...