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Tamoxifen Resistance: Emerging Molecular Targets

Department of Medical Sciences, University of Turin, Turin 10126, Italy
Faculty of Natural Sciences and Mathematics, Universidad del Rosario, Bogotá 11001000, Colombia
Doctoral Program in Biomedical Sciences, Universidad del Rosario, Bogotá 11001000, Colombia
Department of Biosciences and Nutrition, Karolinska Institutet, Huddinge 14183, Sweden
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editor: William Chi-shing Cho
Int. J. Mol. Sci. 2016, 17(8), 1357;
Received: 5 July 2016 / Revised: 10 August 2016 / Accepted: 16 August 2016 / Published: 19 August 2016
(This article belongs to the Collection Advances in Molecular Oncology)
17β-Estradiol (E2) plays a pivotal role in the development and progression of breast cancer. As a result, blockade of the E2 signal through either tamoxifen (TAM) or aromatase inhibitors is an important therapeutic strategy to treat or prevent estrogen receptor (ER) positive breast cancer. However, resistance to TAM is the major obstacle in endocrine therapy. This resistance occurs either de novo or is acquired after an initial beneficial response. The underlying mechanisms for TAM resistance are probably multifactorial and remain largely unknown. Considering that breast cancer is a very heterogeneous disease and patients respond differently to treatment, the molecular analysis of TAM’s biological activity could provide the necessary framework to understand the complex effects of this drug in target cells. Moreover, this could explain, at least in part, the development of resistance and indicate an optimal therapeutic option. This review highlights the implications of TAM in breast cancer as well as the role of receptors/signal pathways recently suggested to be involved in the development of TAM resistance. G protein—coupled estrogen receptor, Androgen Receptor and Hedgehog signaling pathways are emerging as novel therapeutic targets and prognostic indicators for breast cancer, based on their ability to mediate estrogenic signaling in ERα-positive or -negative breast cancer. View Full-Text
Keywords: tamoxifen; breast cancer; G protein-coupled estrogen receptor (GPER); estrogen receptors (ERs); androgen receptor (AR); Hedgehog (HH) signaling pathway; endocrine resistance tamoxifen; breast cancer; G protein-coupled estrogen receptor (GPER); estrogen receptors (ERs); androgen receptor (AR); Hedgehog (HH) signaling pathway; endocrine resistance
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MDPI and ACS Style

Rondón-Lagos, M.; Villegas, V.E.; Rangel, N.; Sánchez, M.C.; Zaphiropoulos, P.G. Tamoxifen Resistance: Emerging Molecular Targets. Int. J. Mol. Sci. 2016, 17, 1357.

AMA Style

Rondón-Lagos M, Villegas VE, Rangel N, Sánchez MC, Zaphiropoulos PG. Tamoxifen Resistance: Emerging Molecular Targets. International Journal of Molecular Sciences. 2016; 17(8):1357.

Chicago/Turabian Style

Rondón-Lagos, Milena, Victoria E. Villegas, Nelson Rangel, Magda C. Sánchez, and Peter G. Zaphiropoulos 2016. "Tamoxifen Resistance: Emerging Molecular Targets" International Journal of Molecular Sciences 17, no. 8: 1357.

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