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Pathway Description
Estramustine Action Pathway
Homo sapiens
Category:
Metabolite Pathway
Sub-Category:
Drug Action
Created: 2023-08-02
Last Updated: 2023-11-27
Estramustine is a nitrogen mustard linked to an estradiol moiety. This drug is used as an antineoplastic agent for the palliative treatment of metastatic and progressive carcinoma of the prostate. The nitrogen mustard moiety gives the molecule its alkylating properties. This alkylation causes DNA strandbreaks or miscoding events. The damage made to DNA leads to the apoptosis of the cancerous cell. Furthermore, this moiety also binds to some microtubule proteins. The estradiol component of the drug gives estramustine the ability to bind more selectively to estrogen receptors. This drug is administered as an oral capsule.
References
Estramustine Pathway References
Wishart DS, Feunang YD, Guo AC, Lo EJ, Marcu A, Grant JR, Sajed T, Johnson D, Li C, Sayeeda Z, Assempour N, Iynkkaran I, Liu Y, Maciejewski A, Gale N, Wilson A, Chin L, Cummings R, Le D, Pon A, Knox C, Wilson M: DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2018 Jan 4;46(D1):D1074-D1082. doi: 10.1093/nar/gkx1037.
Pubmed: 29126136
Ho SM: Estrogens and anti-estrogens: key mediators of prostate carcinogenesis and new therapeutic candidates. J Cell Biochem. 2004 Feb 15;91(3):491-503. doi: 10.1002/jcb.10759.
Pubmed: 14755680
Ferno M, Borg A, Ingvar C, Jonsson PE: Estrogen receptor and binding site for estramustine in metastatic malignant melanoma. Anticancer Res. 1987 Jul-Aug;7(4B):741-3.
Pubmed: 3314674
Tew KD: The mechanism of action of estramustine. Semin Oncol. 1983 Sep;10(3 Suppl 3):21-6.
Pubmed: 6364362
Moraga D, Rivas-Berrios A, Farias G, Wallin M, Maccioni RB: Estramustine-phosphate binds to a tubulin binding domain on microtubule-associated proteins MAP-2 and tau. Biochim Biophys Acta. 1992 May 22;1121(1-2):97-103. doi: 10.1016/0167-4838(92)90342-b.
Pubmed: 1599956
Stearns ME, Wang M, Sousa O: Evidence that estramustine binds MAP-1A to inhibit type IV collagenase secretion. J Cell Sci. 1991 Jan;98 ( Pt 1):55-63. doi: 10.1242/jcs.98.1.55.
Pubmed: 1647395
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