ES-FLI1 is an oncogenic fusion protein found in Ewing’s sarcoma, a crime syndicate of undifferentiated tumors that occur throughout the body.
The binding of RNA helicase A (RHA) to ES-FLI1 promotes its oncogenic function. The binding of RNA helicase A (RHA) to ES-FLI1 promotes its oncogenic function. YK-4-279 is an inhibitor of protein-protein interactions between ES-FLI1 and RHA. At 10 µM, YK-4-279 blocks RHA binding to ES-FLI1 and induces apoptosis of a panel of Ewing’s sarcoma tumor cell lines with IC50 values ranging from 0.5-2 µM.
YK-4-279 is an inhibitor of protein-protein interactions between ES-FLI1 and RHA. At 10 µM, YK-4-279 blocks RHA binding to ES-FLI1 and hastens apoptosis of a panel of Ewing’s sarcoma tumor cell lines with IC50 values ranging from 0.5 to 2 µM.1 At 1.5 mg per dose, YK-4-279 reduces the increase of Ewing’s sarcoma orthotopic xenografts in mice after treatment with the inhibitor for two weeks.
YK-4-279 also decreased ERG and ETV1 downstream target mRNA and protein expression in ETV1-fusion positive LNCaP and ERG fusion positive VCaP cells. YK-4-279 reduced the motility of LNCaP cells in a scratch assay and the invasive phenotype of both LNCaP and VCaP cells in a HUVEC invasion assay. Fusion-negative PC3 cells were unresponsive to YK-4-279. SiRNA mediated ERG knockdown in VCaP cells resulted in a loss of drug responsiveness.
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