A small molecule inhibitor of ETV1, YK-4-279, prevents prostate cancer growth and metastasis in a mouse xenograft model

ETV1 的小分子抑制剂 YK-4-279 可在小鼠异种移植模型中预防前列腺癌的生长和转移

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作者:Said Rahim, Tsion Minas, Sung-Hyeok Hong, Sarah Justvig, Haydar Çelik, Yasemin Saygideger Kont, Jenny Han, Abraham T Kallarakal, Yali Kong, Michelle A Rudek, Milton L Brown, Bhaskar Kallakury, Jeffrey A Toretsky, Aykut Üren

Background

The erythroblastosis virus E26 transforming sequences (ETS) family of transcription factors consists of a highly conserved group of genes that play important roles in cellular proliferation, differentiation, migration and invasion. Chromosomal translocations fusing ETS factors to promoters of androgen responsive genes have been found in prostate cancers, including the most clinically aggressive forms. ERG and ETV1 are the most commonly translocated ETS proteins. Over-expression of these proteins in prostate cancer cells

Conclusion

Our results demonstrate that YK-4-279 is a potent inhibitor of ETV1 and inhibits both the primary tumor growth and metastasis of fusion positive prostate cancer xenografts. Therefore, YK-4-279 or similar compounds may be evaluated as a potential therapeutic tool for treatment of human prostate cancer at different stages.

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