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Targeting ERα degradation by L-Tetrahydropalmatine provides a novel strategy for breast cancer treatment
- Source :
- International Journal of Biological Sciences
- Publication Year :
- 2020
- Publisher :
- Ivyspring International Publisher, 2020.
-
Abstract
- The incidence and mortality of breast cancer (BCa) are the highest among female cancers. There are approximate 70% BCa that are classified as estrogen receptor alpha (ERα) positive. Therefore, targeting ERα is the most significantly therapeutic schedule. However, patients with breast cancer develop resistance to ERα or estrogen (E2) antagonists such as fulvestrant and tamoxifen. In the present study, we found that L-Tetrahydropalmatine (L-THP) significantly suppressed cell proliferation in ERα+ BCa cells via inducing cell cycle arrest rather than apoptosis. Additionally, L-THP enhanced the sensitivity of ERα+ BCa cells to tamoxifen and fulvestrant. Mechanically, the application of L-THP promotes ERα degradation through accumulating ubiquitin chains on ERα. Overexpressing ERα abrogates L-THP induced-antiproliferation in ERα+ BCa cells. Collectively, our work indicates that L-THP may represent a potentially novel therapeutic medicine for ERα+ breast cancer patient.
- Subjects :
- L-THP
Models, Molecular
Cell cycle checkpoint
Antineoplastic Agents, Hormonal
Cell Survival
Protein Conformation
medicine.drug_class
proliferation
Berberine Alkaloids
Breast Neoplasms
Applied Microbiology and Biotechnology
03 medical and health sciences
breast cancer
Breast cancer
Cell Line, Tumor
medicine
Humans
skin and connective tissue diseases
Fulvestrant
Molecular Biology
Ecology, Evolution, Behavior and Systematics
ERα
030304 developmental biology
0303 health sciences
Cell growth
business.industry
Estrogen Antagonists
Estrogen Receptor alpha
Cell Biology
Cell cycle
medicine.disease
Gene Expression Regulation, Neoplastic
Tamoxifen
Drug Resistance, Neoplasm
Estrogen
Cancer research
Dopamine Antagonists
cell cycle
Female
business
Estrogen receptor alpha
Research Paper
Developmental Biology
medicine.drug
Subjects
Details
- ISSN :
- 14492288
- Volume :
- 16
- Database :
- OpenAIRE
- Journal :
- International Journal of Biological Sciences
- Accession number :
- edsair.doi.dedup.....e31d4e99dd177825faf06fe179c2aa59