Human estrogen receptor alpha (ERα) targeted cyclic peptides inhibit cell growth and induce apoptosis in MCF-7 cells

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dc.authorscopusidEngin Ulukaya / 6602927353
dc.authorscopusidHuri Dedeakayoğulları / 57191334242
dc.authorscopusidMuradiye Acar / 50261019400
dc.authorwosidEngin Ulukaya / K-5792-2018
dc.authorwosidHuri Dedeakayoğulları / IWR-0215-2023
dc.authorwosidMuradiye Acar / B-6537-2019
dc.contributor.authorŞentürk, Hilal
dc.contributor.authorDedeakayoğulları, Huri
dc.contributor.authorMarion, İlke U.
dc.contributor.authorÖzçubukçu, Salih
dc.contributor.authorKesici, Mehmet S.
dc.contributor.authorBeyge, Şeyma Ünsal
dc.contributor.authorAcar, Muradiye
dc.contributor.authorGenel, Merve Erkısa
dc.contributor.authorAkbaş, Fahri
dc.contributor.authorUlukaya, Engin
dc.date.accessioned2025-04-18T10:18:26Z
dc.date.available2025-04-18T10:18:26Z
dc.date.issued2024
dc.departmentİstinye Üniversitesi, Tıp Fakültesi, Temel Tıp Bilimleri Bölümü
dc.description.abstractObjectives Human estrogen receptor alpha (ER alpha) is considered an important target, especially in the treatment of breast cancer, as it has a vital role in cancer development. ER alpha-targeted therapies generally target the ligand binding domain (LBD) of ER alpha. However, over time, cells develop resistance to this mechanism alternative approaches to inhibit ER alpha activity target ER alpha-DNA or ER alpha-cofactor interactions. Inhibitors of ER alpha-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 ER alpha. 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 ER alpha-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 ER alpha, 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.
dc.identifier.citationŞentürk, H., Dedeakayoğulları, H., Marion, İ. U., Özçubukçu, S., Kesici, M. S., Ünsal Beyge, Ş., ... & Ulukaya, E. (2024). Human estrogen receptor alpha (ERα) targeted cyclic peptides inhibit cell growth and induce apoptosis in MCF-7 cells. Turkish Journal of Biochemistry, 49(4), 542-550.
dc.identifier.doi10.1515/tjb-2024-0123
dc.identifier.endpage550
dc.identifier.issn0250-4685
dc.identifier.issn1303-829X
dc.identifier.issue4
dc.identifier.scopus2-s2.0-85202981985
dc.identifier.scopusqualityQ3
dc.identifier.startpage542
dc.identifier.urihttp://dx.doi.org/10.1515/tjb-2024-0123
dc.identifier.urihttps://hdl.handle.net/20.500.12713/7017
dc.identifier.volume49
dc.identifier.wosWOS:001271127200001
dc.identifier.wosqualityQ4
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.institutionauthorDedeakayoğulları, Huri
dc.institutionauthorAcar, Muradiye
dc.institutionauthorUlukaya, Engin
dc.institutionauthoridEngin Ulukaya / 0000-0003-4875-5472
dc.institutionauthoridMuradiye Acar / 0000-0003-4357-5229
dc.language.isoen
dc.publisherWalter de gruyter GMBH
dc.relation.ispartofTurkish journal of biochemistr
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.relation.tubitak223S648
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectApoptosis
dc.subjectBreast Cancer
dc.subjectCoactivator Binding Inhibitors
dc.subjectHelix-Stabilized Cyclic Peptides
dc.subjectHuman Estrogen Receptor Alpha
dc.titleHuman estrogen receptor alpha (ERα) targeted cyclic peptides inhibit cell growth and induce apoptosis in MCF-7 cells
dc.typeArticle

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