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• W3106991775 abstract "Despite intense research, breast cancer remains the leading cause of cancer-related death in women worldwide, being estrogen receptor-positive (ER + ) the most common subtype. Nowadays, aromatase inhibitors (AIs), the selective estrogen receptor modulator (SERM) tamoxifen and the selective estrogen receptor down-regulator (SERD) fulvestrant are used as therapeutic options for ER + breast cancer, since they interfere directly with the production of estrogens and with the activation of estrogen-dependent signaling pathways . Despite the success of these treatments, the occurrence of resistance limits their clinical efficacy, demanding the development of novel therapies. Recently, multi-target compounds emerged as promising therapeutic strategies for ER + breast cancer, as they can potentially modulate several important targets simultaneously. In line with this, in this work, the anti-cancer properties and multi-target action of 1,1-Bis(4-hydroxyphenyl)-2-phenylbut-1-ene, tamoxifen bisphenol (1,1-BHPE), were evaluated in an ER + breast cancer cell model (MCF-7aro cells). Molecular docking analysis predicted that 1,1-BHPE was able to bind to aromatase , ERα and ERβ. In vitro studies showed that, although it did not present anti-aromatase activity, 1,1-BHPE reduced aromatase protein levels and interfered with ERα and ERβ signaling pathways, acting as an ERα antagonist and inducing ERβ up-regulation. Through these mechanisms, 1,1-BHPE was able to impair breast cancer growth and induce apoptosis. This represents an important therapeutic advantage because the main players responsible for estrogen production and signaling are modulated by a single compound. To the best of our knowledge, this is the first study describing the anti-cancer properties of 1,1-BHPE as a multi-target compound specific for ER + breast cancer. • This is the first in vitro study describing the anti-cancer properties of 1,1-Bis(4-hydroxyphenyl)-2-phenylbut-1-ene (1,1-BHPE), also known as tamoxifen bisphenol. • 1,1-BHPE impaired growth and induced apoptosis of ER + breast cancer cells. • This compound targets aromatase by reducing its protein levels on cancer cells. • It also modulates ER signalling pathways, by acting as an ERα antagonist and inducing ERβ up-regulation. • 1,1-BHPE act as a specific multi-target compound in ER + breast cancer cells." @default.
• W3106991775 created "2020-12-07" @default.
• W3106991775 creator A5027411511 @default.
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• W3106991775 date "2021-02-01" @default.
• W3106991775 modified "2023-10-01" @default.
• W3106991775 title "Discovery of a multi-target compound for estrogen receptor-positive (ER+) breast cancer: Involvement of aromatase and ERs" @default.
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• W3106991775 doi "https://doi.org/10.1016/j.biochi.2020.11.023" @default.
• W3106991775 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/33278557" @default.
• W3106991775 hasPublicationYear "2021" @default.
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