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Título del libro: Breast Cancer
Título del capítulo: Novel Breast Cancer Treatment by Targeting Estrogen Receptor-Alpha Stability Using Proteolysis-Targeting Chimeras (PROTACs) Technology

Autores UNAM:
ANGELES CONCEPCION TECALCO CRUZ; JOSUE ORLANDO RAMIREZ JARQUIN; MARINA MACIAS SILVA; MARCELA SOSA GARROCHO;
Autores externos:

Idioma:

Año de publicación:
2022
Palabras clave:

endocrine resistance in breast cancer; estrogen receptor alpha in breast cancer; novel breast cancer treatment; PROTACs; proteolysis-targeting chimeras technology


Resumen:

Approximately 70% of breast cancer cases are estrogen receptor-alphapositive (ERa+). The binding of estradiol to the ligand-binding domain activates ERa. ERa can also be activated via the phosphorylation induced by growth factors. Activated ERa functions as a transcriptional regulator with a pro-tumor activity in breast cancer cells. In recent years, it has been discovered that some proteins can stabilize ERa by inhibiting its degradation via the ubiquitin-proteasome system through several mechanisms, including ERa monoubiquitination, deubiquitination, or phosphorylation, among others. Herein, we review the proteins associated with the inhibition of ERa degradation and discuss the role of proteolysis-targeting chimeras (PROTACs) as promising therapeutic strategies for breast cancer by inducing ERa degradation. The knowledge of the multiple mechanisms that stabilize ERa protein may be central for the development of new PROTACs for novel breast cancer treatments. © 2022 Exon Publications.


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