4-Methoxyestradiol

4-Methoxyestradiol (4-ME), also known as 2-Methoxyestradiol or 2-ME2, is a natural metabolite of estradiol. It is formed in the body by the action of the enzyme catechol-O-methyltransferase on 2-hydroxyestradiol.

Pharmacology

4-Methoxyestradiol has been found to possess antiproliferative and antiangiogenic effects, and it inhibits the growth of cancer cells in laboratory studies. It is thought to exert its effects by binding to tubulin, a protein involved in cell structure and function, and disrupting its normal function.

Clinical significance

4-Methoxyestradiol has been investigated for potential use in the treatment of cancer. It has been studied in clinical trials for the treatment of lung cancer, prostate cancer, and breast cancer, among other types of cancer. However, as of 2021, it has not been approved for medical use.

See also

• Estradiol
• Catechol-O-methyltransferase
• 2-Hydroxyestradiol
• Tubulin

4-Methoxyestradiol Resources
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