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Zebularine is a cell-permeable chemically stable cytidine analog and DNA methylation inhibitor which acts by forming a covalent complex with DNMT. It displays antiangiogenic activity and markedly inhibits vessel formation in different tumor models. It reactivates silenced E-cadherin and potentiates the effects of other epigenetic therapeutics such as vorinistat. Induces differentiation of mesenchymal cells into cardiomyocytes. Inhibits cytidine deaminase (CDD).
1. Frick, L., et al., 1989. Binding of pyrimidin-2-one ribonucleoside by cytidine deaminase as the transition-state analogue 3,4-dihydrouridine and the contribution of the 4-hydroxyl group to its binding affinity. Biochemistry. 28(24): 9423-30. PMID: 2692708
2. Zhou, L., et al., 2002. Zebularine: a novel DNA methylation inhibitor that forms a covalent complex with DNA methyltransferases. Journal of molecular biology. 321(4): 591-9. PMID: 12206775
3. Cheng, Jonathan C., et al., 2003. Inhibition of DNA methylation and reactivation of silenced genes by zebularine. Journal of the National Cancer Institute. 95(5): 399-409. PMID: 12618505
4. Cheng, Jonathan C., et al., 2004. Preferential response of cancer cells to zebularine. Cancer cell. 6(2): 151-8. PMID: 15324698
See how others have used Zebularine. Click on the entry to view the PubMed entry .
PMID: # 15550378 Peng, B. et al. 2005. J. Biol. Chem. 280: 4182-4187.
PMID: # 14729971 Cheng, J.C. et al. 2004. Mol. Cell. Biol. 24: 1270-1278.
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