Genome-wide analysis of the three-way interplay among gene expression, estrogen receptor expression and chemotherapeutic sensitivity in breast cancer

Abstract

The expression of estrogen receptor α (ER) in breast cancers may be indicative of a favorable prognosis and most of these cancers respond to anti-estrogens or aromatase inhibitors. However, ER-positive (ER+) breast cancers receiving anti-hormone and/or chemotherapy sometimes lose their ER expression, which leads to the evolution of the disease to higher aggressiveness and drug resistance. In the present study, an ER-modified signature (EMS) was developed from the expression profile of a chemoresistant MCF-7 breast cancer cell line that lost ER expression during long-term treatment with a chemotherapeutic agent. The EMS could discriminate the ER-negative (ER−) breast cancer cells from the ER+ ones, which included seven pathways essential for the ER− cell development. Furthermore, the EMS indicated a more malignant subgroup of the ER− cells by discriminating the chemoresistant ER− cells from the chemosensitive ones. In addition, the classified chemoresistant ER− patients demonstrated worse prognosis. In conclusion, we developed a new method to discriminate subgroups of ER− breast cancer cells.

New azolyl-derivatives as multitargeting agents against breast cancer and fungal infections: synthesis, biological evaluation and docking study

“…Nevertheless, there is a fall in the cell metabolic activity after this concentration range for compound 5 which discloses the lowest IC 50 comparing 24 to 48 h (68.8 mM). The higher metabolic activity registered after 72 h in the lower concentration range, as a counteraction of the decreasing trend registered after 24 and 48 h mainly for compounds 2 and 5, could be ascribed to chemoresistance mechanisms established by MCF-7 cells 22,23 .…”

Design, Synthesis and Biological Evaluation of Aromatase Inhibitors Based on Sulfonates and Sulfonamides of Resveratrol

“…On the contrary, compound 1j seems to bind the aromatase enzyme better than 1c, showing the best percentage of inhibition (100.43%) and the lower IC50 (2.21 μM), but this behavior is not retained in the cells. This fact could be referred to as chemoresistance mechanisms [59,60].…”