Alysha Higgs
Tamoxifen Outline
I. Introduction Tamoxifen is the “oldest and most prescribed SERM” (10). SERM is selective estrogen receptor modulators. It is used to treat advanced-stage hormone-receptor-positive disease and breast cancer.
a. is a synthetic drug
b. used in mice for inducible cre
c. synthesized by allylation of benzaldehyde and alkylation reaction of anisole and ethers.
d. Binds to estrogen receptors
e. Comes with side effects
II. Background Tamoxifen is used in two different aspects and in order to see this one must know the general information of the drug.
a. Explanation of drug makeup and characteristics
b. Explanation of drug dosage and uses
c. Explanation of how it induces cre
III. Synthesis Tamoxifen was discovered…show more content… Goes into detail about tamoxifen and its effects. The source also talks about the mechanism of action of tamoxifen.
(2) Thrane S.; et al. Estrogen receptor α is the major driving factor for growth in tamoxifen-resistant breast cancer and supported by HER/ERK signaling. Breast Cancer Research and Treatment 2013, 139, 71-80. This source talks about resistance of tamoxifen. The research explored the signaling pathways That drives the resistance. The source also explains the resistance in detail.
(3) Feil S.; et al. Inducible Cre Mice. Gene Knockout Protocols 2009, 530, 343-363. Talks about cre mice, how they are used and what happens. Also mentions the role of tamoxifen plays within the mice.
(4) Shiina I.; et al. Short-step synthesis of tamoxifen and its derivatives via the three-component coupling reaction and migration of the double bond. Tetrahedron Letters 2004, 45(5),
965-967.
This source goes into detail of one of the synthesis of tamoxifen. It goes step by step and gives figures.
(5) Borgatta M.; et al. Shotgun Ecotoxicoproteomics of Daphnia pulex: Biochemical Effects of the
Anticancer Drug Tamoxifen. Journal of Proteome Research 2015, 14,…show more content… It explored the effects of the tamoxifen and shows the adverse effects of the drug.
(6) Zhang F.; et al. Synthesis and Reactivity of a Potential Carcinogenic Metabolite of Tamoxifen:
3,4-Dihydroxytamoxifen-o-quinone. Chemical Research in Toxicology 2000, 13, 53-62. This source gives background on tamoxifen and the side effects. The authors of this source are interested in seeing how those side effects happen other than from hormonal properties. They used the synthesis pf the drug to find other compounds that don’t have such harsh effects.
(7) Darakhshan S.; et al. Tranilast enhances the anti-tumor effects of tamoxifen on human breast cancer cells in vitro. Journal of Biomedical Science 2013, 20:76. This source begins by discussing apoptosis and its effects on cancer cells. Then it discusses the effects of estrogen on breast cancer. Then explains how tamoxifen works and how tamoxifen with tranilast will be more effective.
(8) Sporn M. B. and Lippman S. M. Holland-Frei Cancer Medicine, 6th ed.; Hamilton (ON): BC Decker,
2003.
This sources gives the mechanism of action of tamoxifen.
(9) Lorizio W.; et al. Clinical and biomarker predictors of side effects from tamoxifen. Breast
