Low concentrations of 17β‐estradiol exacerbate tamoxifen resistance in breast cancer treatment through membrane estrogen receptor‐mediated signaling pathways

2021 ◽  
Author(s):  
Zhixiang Xu ◽  
Dimeng Zhao ◽  
Xianyao Zheng ◽  
Bin Huang ◽  
Xuejun Pan ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Estrogen Receptor ◽  
Cancer Treatment ◽  
Signaling Pathways ◽  
Tamoxifen Resistance ◽  
Breast Cancer Treatment ◽  
Low Concentrations ◽  
17Β Estradiol

Aromatase Inhibitors for the Treatment of Breast Cancer: A Journey from the Scratch

2020 ◽  
Vol 20 (17) ◽  
pp. 1994-2004 ◽  
Author(s):  
Pooja Ratre ◽  
Keerti Mishra ◽  
Amit Dubey ◽  
Amber Vyas ◽  
Akhlesh Jain ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Estrogen Receptor ◽  
Cancer Treatment ◽  
Postmenopausal Women ◽  
Aromatase Inhibitors ◽  
3D Structure ◽  
Postmenopausal Breast Cancer ◽  
Breast Cancer Treatment ◽  
Third Generation ◽  
Breast Cancer Chemotherapy

Background: Estrogens are essential for the growth of breast cancer in the case of premenopausal as well as in postmenopausal women. However, most of the breast cancer incidences are reported in postmenopausal women and the concurrent risk surges with an increase in age. Since the enzyme aromatase catalyses essential steps in estrogen biosynthesis, Aromatase Inhibitors (AIs) are effective targeted therapy in patients with Estrogen Receptor positive (ER+) breast cancer. AIs are more effective than Selective Estrogen Receptor Modulators (SERMs) because they block both the genomic and nongenomic activities of ER. Till date, first, second and third-generation AIs have been approved by the FDA. The third-generation AIs, viz. Letrozole, Anastrozole, Exemestane, are currently used in the standard treatment for postmenopausal breast cancer. Methods: Data were collected from Medline, PubMed, Google Scholar, Science Direct through searching of keywords: ‘aromatase’, ‘aromatase inhibitors’, ‘breast cancer’, ‘steroidal aromatase inhibitors’, ‘non-steroidal inhibitors’ and ‘generations of aromatase inhibitors’. Results: In the current scenario of breast cancer chemotherapy, AIs are the most widely used agents which reveal optimum efficacy along with the least side effects. Keeping in view the prominence of AIs in breast cancer therapy, this review covered the detailed description of aromatase including its role in the biosynthesis of estrogen, biochemistry, gene expression, 3D-structure, and information of reported AIs along with their role in breast cancer treatment. Conclusion: AIs are the mainstream solution of the ER+ breast cancer treatment regimen with the continuous improvement of human understanding of the importance of a healthy life of women suffering from breast cancer.

scholarly journals Development, Characterization and In Vitro Evaluation of Paclitaxel and Anastrozole Co-Loaded Liposome

Processes ◽  
2020 ◽  
Vol 8 (9) ◽  
pp. 1110
Author(s):  
Minh Thanh Vu ◽  
Dinh Tien Dung Nguyen ◽  
Ngoc Hoi Nguyen ◽  
Van Thu Le ◽  
The Nam Dao ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Estrogen Receptor ◽  
Combination Therapy ◽  
Cancer Treatment ◽  
Cancer Cells ◽  
Breast Cancer Treatment ◽  
In Vitro Cytotoxicity ◽  
Cytotoxicity Studies ◽  
Combined Drugs

Paclitaxel (PTX) and anastrozole (ANA) have been frequently applied in breast cancer treatment. PTX is well-known for its anti-proliferative effect meanwhile ANA has just been discovered to act as an estrogen receptor α (ERα) ligand. The combination therapy of PTX and ANA is expected to improve treating efficiency, as ANA would act as a ligand binding with the ERα gene expressed in breast cancer cells and thereafter PTX would inhibit the division and cause death to those cancer cells. In this study, liposome-based nanocarriers (LP) were developed for co-encapsulation of PTX and ANA to improve the efficacy of the combined drugs in an Estrogen receptor-responsive breast cancer study. PTX-ANA co-loaded LP was prepared using thin lipid film hydration method and was characterized for morphology, size, zeta potential, drug encapsulation and in vitro drug release. In addition, cell proliferation (WST assay) and IN Cell Analyzer were used for in vitro cytotoxicity studies on a human breast cancer cell line (MCF-7). Results showed that the prepared LP and PTX-ANA-LP had spherical vesicles, with a mean particle size of 170.1 ± 13.5 nm and 189.0 ± 22.1 nm, respectively. Controlled and sustained releases were achieved at 72 h for both of the loaded drugs. The in vitro cytotoxicity study found that the combined drugs showed higher toxicity than each single drug separately. These results suggested a new approach to breast cancer treatment, consisting of the combination therapy of PTX and ANA in liposomes based on ER response.

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