Encyclopedia of Cancer

Living Edition
| Editors: Manfred Schwab

Methoxyestradiol

Living reference work entry
DOI: https://doi.org/10.1007/978-3-642-27841-9_3681-2

Synonyms

Definition

2-Methoxyestradiol (2ME2) is a naturally occurring substance that is produced when the hormone estradiol is processed (metabolized) in the body. 2ME2 prevents both tumor growth (antiproliferative) and the formation of new blood vessels that tumors require to grow (antiangiogenic). Although 2ME2 is derived from estradiol, it binds poorly to estrogen receptors. On the contrary, it binds directly to a protein called tubulin, which is involved in cell division. This binding not only interferes with cell division (cell growth) but also inhibits hypoxia inducible factor-1 (HIF-1), an important factor for tumor cell survival. Additionally, 2ME2 has been reported to preferentially kill tumor cells, sparing normal cells, by causing reactive oxygen species (ROS) accumulation in cancer cells.

2ME2 under the trademark Panzem® (EntreMed Inc., Rockville, MD) is currently in Phase I/II clinical studies to investigate its safety and efficacy...

Keywords

Vascular Endothelial Growth Factor Arsenic Trioxide Vascular Endothelial Growth Factor Secretion Microtubule Disruption Colchicine Binding Site 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.
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References

  1. Kang SH, Cho HT, Devi S et al (2006) Antitumor effect of 2-methoxyestradiol in a rat orthotopic brain tumor model. Cancer Res 66:11991–11997CrossRefPubMedGoogle Scholar
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  3. Mabjeesh NJ, Escuin D, LaVallee TM et al (2003) 2ME2 inhibits tumor growth and angiogenesis by disrupting microtubules and dysregulating HIF. Cancer Cell 3:363–375CrossRefPubMedGoogle Scholar
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Copyright information

© Springer-Verlag Berlin Heidelberg 2015

Authors and Affiliations

  1. 1.Department of Hematology/OncologyWinship Cancer Institute, Emory UniversityAtlantaUSA