Description
Estramustine is a derivative of estradiol and the nitrogen mustard mechlorethamine that is clinically used to treat prostate cancer. Estramustine primarily exerts its anticancer chemotherapeutic activity through antimitotic actions. Estramustine acetylates microtubules, stabilizing them and inducing depolymerization, resulting in apoptosis across a variety of cancer cell types. Estramustine also increases DNA fragmentation in glioma cells and tumors (in vivo), but not in normal tissue.
References
Matsumoto K, Tanaka N, Hayakawa N, et al. Efficacy of estramustine phosphate sodium hydrate (EMP) monotherapy in castration-resistant prostate cancer patients: report of 102 cases and review of literature. Med Oncol. 2013 Dec;30(4):717. PMID: 24005812.
Mohan R, Panda D. Kinetic stabilization of microtubule dynamics by estramustine is associated with tubulin acetylation, spindle abnormalities, and mitotic arrest. Cancer Res. 2008 Aug 1;68(15):6181-9. PMID: 18676841.
Yoshida D, Hoshino S, Shimura T, et al. Drug-induced apoptosis by anti-microtubule agent, estramustine phosphate on human malignant glioma cell line, U87MG; in vitro study. J Neurooncol. 2000 Apr;47(2):133-40. PMID: 10982154.
Panda D, Miller HP, Islam K, et al. Stabilization of microtubule dynamics by estramustine by binding to a novel site in tubulin: a possible mechanistic basis for its antitumor action. Proc Natl Acad Sci U S A. 1997 Sep 30;94(20):10560-4. PMID: 9380674.
Punzi JS, Duax WL, Strong P, et al. Molecular conformation of estramustine and two analogues. Mol Pharmacol. 1992 Mar;41(3):569-76. PMID: 1545778.
