Selective Non-nucleoside Inhibitors of Human DNA Methyltransferases Active in Cancer Including in Cancer Stem Cells

Valente, Sérgio; Liu, Yiwei; Schnekenburger, Michaël; Zwergel, Clemens; Cosconati, Sandro; Gros, Christina; Tardugno, Maria; Labella, Donatella; Florean, Cristina; Minden, Steven; Hashimoto, Hideharu; Chang, Yanqi; Zhang, Xing; Kirsch, Gilbert; Novellino, Ettore; B. Arimondo, Paola; Miele, Evelina; Ferretti, Elisabetta; Gulino, Alberto; Diederich, Marc; Cheng, Xiaodong; Mai, Antonello

doi:10.1021/jm4012627

Public

Selective Non-nucleoside Inhibitors of Human DNA Methyltransferases Active in Cancer Including in Cancer Stem Cells

Published in Journal of Medicinal Chemistry • Jan 4, 2014

Authors:

Sérgio Valente

Yiwei Liu

Michaël Schnekenburger

Abstract

DNA methyltransferases (DNMTs) are important enzymes involved in epigenetic control of gene expression and represent valuable targets in cancer chemotherapy. A number of nucleoside DNMT inhibitors (DNMTi) have been studied in cancer, including in cancer stem cells, and two of them (azacytidine and d...

Subject

Methyltransferase

Decitabine

Azacitidine

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