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2-Methoxyestradiol


2-Methoxyestradiol 2-ME2 is a natural metabolite of estradiol As an experimental drug candidate, it is being developed under the tradename of Panzem It prevents the formation of new blood vessels that tumors need in order to grow angiogenesis, hence it is an angiogenesis inhibitor

It also acts as a vasodilator

2-ME2 is derived from estradiol, although it binds poorly 2000-fold lower activational potency to known estrogen receptors However, 2-ME2 retains activity as a high-affinity agonist of the GPER GPR30

It induces apoptosis in some cancer cell lines

It has undergone Phase 1 clinical trials against breast cancer

A phase II trial of 18 advanced ovarian cancer patients reported encouraging results in October 2007

Preclinical models also suggest that 2-ME2 could also be effective against inflammatory diseases such as rheumatoid arthritis Several studies have been conducted showing 2-ME2 is a microtubule-inhibitor and effective against prostate cancer in rodents

As of 2015, all clinical development of 2-ME2 has been suspended or discontinued

See also

  • 2-Hydroxyestradiol
  • 2-Methoxyestrone
  • 4-Methoxyestradiol
  • 4-Methoxyestrone
  • 17α-Epiestriol
  • MP-2001

References

  1. ^ EntreMed's Product Information Site Archived May 4, 2005, at the Wayback Machine
  2. ^ Pribluda VS, Gubish ER, Lavallee TM, Treston A, Swartz GM, Green SJ 2000 "2-Methoxyestradiol: an endogenous antiangiogenic and antiproliferative drug candidate" Cancer Metastasis Reviews 19 1-2: 173–9 doi:101023/a:1026543018478 PMID 11191057 
  3. ^ Sibonga JD, Lotinun S, Evans GL, Pribluda VS, Green SJ, Turner RT March 2003 "Dose-response effects of 2-methoxyestradiol on estrogen target tissues in the ovariectomized rat" Endocrinology 144 3: 785–92 doi:101210/en2002-220632 PMID 12586754 
  4. ^ Thekkumkara T, Snyder R, Karamyan VT 2016 "Competitive Binding Assay for the G-Protein-Coupled Receptor 30 GPR30 or G-Protein-Coupled Estrogen Receptor GPER" Methods in Molecular Biology 1366: 11–7 doi:101007/978-1-4939-3127-9_2 PMID 26585123 
  5. ^ LaVallee TM, Zhan XH, Johnson MS, Herbstritt CJ, Swartz G, Williams MS, Hembrough WA, Green SJ, Pribluda VS January 2003 "2-methoxyestradiol up-regulates death receptor 5 and induces apoptosis through activation of the extrinsic pathway" Cancer Research 63 2: 468–75 PMID 12543804 
  6. ^ "EntreMed Presents Results for Panzem® NCD Phase 2 Ovarian Cancer Study" Archived from the original on July 17, 2012 
  7. ^ Lakhani NJ, Sarkar MA, Venitz J, Figg WD February 2003 "2-Methoxyestradiol, a promising anticancer agent" Pharmacotherapy 23 2: 165–72 doi:101592/phco23216532088 PMID 12587805 
  8. ^ "2-Methoxyestradiol - CASI Pharmaceuticals" Adis Insight Retrieved 2 March 2017 

External links

  • Chemical Information and Structure from the Comparative Toxicogenomics Database
  • 2-Methoxyestradiol 4 journal refs as URLs


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