3-Deazaneplanocin A Explained

3-Deazaneplanocin A (DZNep, C-c3Ado) is a drug which acts as both a S-adenosylhomocysteine synthesis inhibitor and also a histone methyltransferase EZH2 inhibitor. Studies have shown that it has effects in vitro against a variety of different tumor cell lines.^{[1] [2] [3] [4] [5]}

In studies on mice, the drug was also found to be effective for the treatment of Ebola virus disease,^[6] apparently interfering with the Ebola viruses ability to block interferon production, thus restoring the ability of immune system to rid the body of ebolavirus.^{[7] [8]}

Notes and References

1. Glazer. R.I.. Knode, M.C.. Tseng, C.K.. Haines, D.R.. Marquez, V.E.. 1986. 3-Deazaneplanocin A: a new inhibitor of S-adenosylhomocysteine synthesis and its effects in human colon carcinoma cells. Biochemical Pharmacology. Elsevier. 35. 24. 4523–7. 10.1016/0006-2952(86)90774-4 . 3790170.
2. Fiskus. W.. Wang. Y.. Sreekumar. A.. Buckley. K. M.. Shi. H.. Jillella. A.. Ustun. C.. Rao. R.. Fernandez. P.. Chen. J.. Balusu. R.. Koul. S.. Atadja. P.. Marquez. V. E.. Bhalla. K. N.. Combined epigenetic therapy with the histone methyltransferase EZH2 inhibitor 3-deazaneplanocin A and the histone deacetylase inhibitor panobinostat against human AML cells. Blood. 114. 13. 2009. 2733–2743. 19638619. 2756128. 10.1182/blood-2009-03-213496.
3. Kikuchi. Junko. Takashina. Taichi. Kinoshita. Ichiro. Kikuchi. Eiki. Shimizu. Yasushi. Sakakibara-Konishi. Jun. Oizumi. Satoshi. Marquez. Victor E.. Nishimura. Masaharu. Dosaka-Akita. Hirotoshi. Epigenetic therapy with 3-deazaneplanocin A, an inhibitor of the histone methyltransferase EZH2, inhibits growth of non-small cell lung cancer cells. Lung Cancer. 78. 2. 2012. 138–143. 3472089. 22925699. 10.1016/j.lungcan.2012.08.003.
4. Liang. Shen. 2013. 3-Deazaneplanocin A is a Promising Therapeutic Agent for Ovarian Cancer Cells . Asian Pacific Journal of Cancer Prevention. 14. 5. 1513-7368.
5. Fujiwara. T.. Saitoh. H.. Inoue. A.. Kobayashi. M.. Okitsu. Y.. Katsuoka. Y.. Fukuhara. N.. Onishi. Y.. Ishizawa. K.. Ichinohasama. R.. Harigae. H.. 3-Deazaneplanocin A (DZNep), an Inhibitor of S-Adenosylmethionine-dependent Methyltransferase, Promotes Erythroid Differentiation. Journal of Biological Chemistry. 289. 12. 2014. 8121–8134. 3961643. 24492606. 10.1074/jbc.M114.548651. free.
6. 10.1086/514316. Antiviral Drug Therapy of Filovirus Infections: S-Adenosylhomocysteine Hydrolase Inhibitors Inhibit Ebola Virus in Vitro and in a Lethal Mouse Model. The Journal of Infectious Diseases. 179. S240–7. 1999. Huggins . J. . Zhang . Z. X. . Bray . M. . 9988190. free.
7. 12076759. 2002. Bray. M. 3-deazaneplanocin a induces massively increased interferon-alpha production in Ebola virus-infected mice. Antiviral Research. 55. 1. 151–9. Raymond. J. L.. Geisbert. T. Baker. R. O. . 10.1016/s0166-3542(02)00018-9.
8. 25246419. 4216250. 2014. Shuchman. M. Could interferon help treat Ebola?. Canadian Medical Association Journal. 10.1503/cmaj.109-4906 . 186 . 16. 1204.