Background
GSK2879552 is a selective, orally bioavailable, mechanism-based inactivator of lysine-specific demethylase 1 (LSD1)/corepressor for element-1-silencing transcription factor (CoREST) activity.1 Inhibition of LSD1 via GSK2879552 has been shown to enhance H3K4 methylation and to increase the expression of tumor-suppressor genes.1,2 GSK2879552 demonstrates anti-proliferative growth effects (EC50s = 2-240 nM) in AML cell lines and is currently under clinical evaluation for cancer treatment.1,3
1.Mohammad, H.P., Smitheman, K.N., Kamat, C.D., et al.A DNA hypomethylation signature predicts antitumor activity of LSD1 inhibitors in SCLCCancer Cell28(1)57-69(2015)
2.Maes, T., Mascaró, C., Ortega, A., et al.KDM1 histone lysine demethylases as targets for treatments of oncological and neurodegenerative diseaseEpigenomics7(4)609-626(2015)
3.Zheng, Y.C., Yu, B., Jiang, G.Z., et al.Irreversible LSD1 inhibitors: Application of tranylcypromine and its derivatives in cancer treatmentCurr. Top. Med. Chem.16(19)2179-2188(2016)
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