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. 2011 Apr 29;6(4):e19343. doi: 10.1371/journal.pone.0019343

Figure 2. YK-4-279 inhibits ERG and ETV1 transcriptional activity.

Figure 2

a) Binding kinetics of YK-4-279 to ERG and ETV1 was determined by surface plasmon resonance. YK-4-279 bound to ERG and ETV1 with a KD of 11.7 µM and 17.9 µM respectively. SPR sensorgrams are provided in supplementary figures (Fig. S1). b) A luciferase assay was performed in Cos-7 cells co-transfected with ERG and an Id-2 reporter luciferase construct. Id-2 promoter activity was decreased upon YK-4-279 treatment without affecting ERG protein levels. * ; p<0.001. c) VCaP cells were treated with 50 nM siERG or 10 µM YK-4-279 for 48 hours and mRNA and protein expression levels of ERG targets were evaluated. YK-4-279 treatment resulted in decreased expression of PLAU, ADAM19 and PLAT mRNA. PLAU and PLAT protein levels were decreased as well. Results were comparable to those obtained by siRNA mediated ERG knockdown. d) LNCaP cells were treated with 1 µM YK-4-279 and ETV1 target gene levels were evaluated. YK-4-279 treatment resulted in decreased gene expression of MMP13 without significant reduction in ETV1 levels. * ; p<0.01.