3-Deazaneplanocin A

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3-Deazaneplanocin A
3-Deazaneplanocin A.svg
Identifiers
102052-95-9
ChemSpider 65874
Jmol-3D images Image
PubChem 73087
Properties
C12H14N4O3
Molar mass 262.265
Except where noted otherwise, data is given for materials in their standard state (at 25 °C (77 °F), 100 kPa)
Infobox references

3-Deazaneplanocin A (DZNep) 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 in vitro against a variety of different tumor cell lines.[1][2][3][4][5]

In studies on mice, 3-deazaneplanocin A 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 which usually allows it to evade immune responses.[7][8]

References[edit]

  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). doi:10.1016/0006-2952(86)90774-4. 
  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. (2009). "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): 2733–2743. doi:10.1182/blood-2009-03-213496. PMC 2756128. PMID 19638619.  edit
  3. ^ Kikuchi, Junko; Takashina, Taichi; Kinoshita, Ichiro; Kikuchi, Eiki; Shimizu, Yasushi; Sakakibara-Konishi, Jun; Oizumi, Satoshi; Marquez, Victor E.; Nishimura, Masaharu; Dosaka-Akita, Hirotoshi (2012). "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): 138–143. doi:10.1016/j.lungcan.2012.08.003. PMC 3472089. PMID 22925699.  edit
  4. ^ Liang, Shen (2013). "3-Deazaneplanocin A is a Promising Therapeutic Agent for Ovarian Cancer Cells". Asian Pacific Journal of Cancer Prevention 14 (5). ISSN 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. (2014). "3-Deazaneplanocin A (DZNep), an Inhibitor of S-Adenosylmethionine-dependent Methyltransferase, Promotes Erythroid Differentiation". Journal of Biological Chemistry 289 (12): 8121–8134. doi:10.1074/jbc.M114.548651. PMC 3961643. PMID 24492606.  edit
  6. ^ Huggins, J.; Zhang, Z. X.; Bray, M. (1999). "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. doi:10.1086/514316. PMID 9988190.  edit
  7. ^ Bray, M; Raymond, J. L.; Geisbert, T; Baker, R. O. (2002). "3-deazaneplanocin a induces massively increased interferon-alpha production in Ebola virus-infected mice". Antiviral research 55 (1): 151–9. PMID 12076759.  edit
  8. ^ Shuchman, M (2014). "Could interferon help treat Ebola?". Canadian Medical Association Journal 186: 1204. doi:10.1503/cmaj.109-4906. PMID 25246419.  edit