Human estrogen receptor alpha (ERα) targeted cyclic peptides inhibit cell growth and induce apoptosis in MCF-7 cells
Objectives: Human estrogen receptor alpha (ERα) is considered an important target, especially in the treatment of breast cancer, as it has a vital role in cancer development. ERα-targeted therapies generally target the ligand binding domain (LBD) of ERα. However, over time, cells develop resistance to this mechanism alternative approaches to inhibit ERα activity target ERα–DNA or ERα–cofactor interactions. Inhibitors of ERα–cofactor interactions are designed by targeting the hydrophobic hollow region of the receptor box LXXLL motif. Methods: In this context, helix-stabilized cyclic peptides (SPs) designed with in silico approaches were obtained by solid phase peptide synthesis. The effects of SPs on MCF-7 cells were examined with MTT and ATP, and qPCR and flow cytometry were used for further analysis. Results: Our results demonstrated that the SPs were effective only in MCF-7 cells expressing ERα. In addition, cyclic peptide combinations (SPCs) showed anti-proliferative and toxic effects on MCF-7 cells. The impact of SPCs with the highest inhibitory effect in MCF-7 cells on ERα-related genes and markers of apoptosis was revealed. Moreover, the flow cytometry analysis result used to examine apoptotic cells proved the apoptosis of SPCs in MCF-7 cells. Conclusions: These findings suggest that our novel SPs, which inhibit coactivator interactions of ERα, induce apoptosis of MCF-7 cells. Thus, considering this strong effect of SPs in the inhibition of receptors, it is pointed out that they can be further developed as an alternative to current clinical treatments or as an auxiliary approach in the generating of new targeted peptide-based therapies.
- Location
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Deutsche Nationalbibliothek Frankfurt am Main
- Extent
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Online-Ressource
- Language
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Englisch
- Bibliographic citation
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Human estrogen receptor alpha (ERα) targeted cyclic peptides inhibit cell growth and induce apoptosis in MCF-7 cells ; volume:49 ; number:4 ; year:2024 ; pages:542-550 ; extent:09
Turkish journal of biochemistry ; 49, Heft 4 (2024), 542-550 (gesamt 09)
- Creator
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Şentürk, Hilal
Dedeakayoğulları, Huri
Marion, İlke U.
Özçubukçu, Salih
Kesici, Mehmet S.
Ünsal Beyge, Şeyma
Acar, Muradiye
Erkısa Genel, Merve
Akbaş, Fahri
Ulukaya, Engin
- DOI
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10.1515/tjb-2024-0123
- URN
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urn:nbn:de:101:1-2408311747314.529095475440
- Rights
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Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
- Last update
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15.08.2025, 7:24 AM CEST
Data provider
Deutsche Nationalbibliothek. If you have any questions about the object, please contact the data provider.
Associated
- Şentürk, Hilal
- Dedeakayoğulları, Huri
- Marion, İlke U.
- Özçubukçu, Salih
- Kesici, Mehmet S.
- Ünsal Beyge, Şeyma
- Acar, Muradiye
- Erkısa Genel, Merve
- Akbaş, Fahri
- Ulukaya, Engin
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Membrane estrogen receptor-α levels predict estrogen-induced ERK1/2 activation in MCF-7 cells
Gold nanoparticles conjugated with resveratrol induce cell cycle arrest in MCF-7 cell lines
Estrogen-like activity of aqueous extract from Agrimonia pilosa Ledeb. in MCF-7 cells
The triterpenoids of Hibiscus syriacus induce apoptosis and inhibit cell migration in breast cancer cells
Decursin and decursinol angelate inhibit estrogen-stimulated and estrogen-independent growth and survival of breast cancer cells
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Ligand-free estrogen receptor activity complements IGF1R to induce the proliferation of the MCF-7 breast cancer cells
Membrane estrogen receptor-α levels predict estrogen-induced ERK1/2 activation in MCF-7 cells
Gold nanoparticles conjugated with resveratrol induce cell cycle arrest in MCF-7 cell lines
Estrogen-like activity of aqueous extract from Agrimonia pilosa Ledeb. in MCF-7 cells
The triterpenoids of Hibiscus syriacus induce apoptosis and inhibit cell migration in breast cancer cells
Decursin and decursinol angelate inhibit estrogen-stimulated and estrogen-independent growth and survival of breast cancer cells
Statins inhibit proliferation and induce apoptosis in triple-negative breast cancer cells
Artemisia Capillaris leaves inhibit cell proliferation and induce apoptosis in hepatocellular carcinoma
Prosopis juliflora leave extracts induce cell death of MCF-7, HepG2, and LS-174T cancer cell lines
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