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

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dc.authorid0000-0002-3908-7778
dc.authorid0000-0003-2706-9625
dc.authorid0000-0002-9083-656X
dc.authorid0000-0001-5981-1391
dc.authorid0000-0001-6281-5537
dc.authorid0000-0003-4357-5229
dc.authorid0000-0002-3127-742X
dc.authorid0000-0002-3837-250X
dc.authorid0000-0001-9487-4769
dc.authorid0000-0003-4875-5472
dc.contributor.authorŞentürk, Hilal
dc.contributor.authorDedeakayoğulları, Huri
dc.contributor.authorUğur Marion, İlke
dc.contributor.authorÖzçubukçu, Salih
dc.contributor.authorKesici, Mehmet Seçkin
dc.contributor.authorÜnsal Beyge, Şeyma
dc.contributor.authorAcar, Muradiye
dc.contributor.authorErkısa Genel, Merve
dc.contributor.authorAkbaş, Fahri
dc.contributor.authorUlukaya, Engin
dc.date.accessioned2024-08-02T12:53:26Z
dc.date.available2024-08-02T12:53:26Z
dc.date.issued2024
dc.departmentFakülteler, Tıp Fakültesi, Temel Tıp Bilimleri Bölümü, Tıbbi Biyokimya Ana Bilim Dalı
dc.description.abstractObjectives: 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 in teractions. 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 effec tive 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.
dc.description.sponsorshipHealth Institutes of Turkey (TUSEB) -- 12162
dc.identifier.citationŞentürk, H., Dedeakayoğulları, H., Uğur Marion, İ., Özçubukçu, S., Kesici, M. S., Ünsal Beyge, Ş., Acar, M., Erkısa Genel, M., Akbaş, F., & 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), pp. 542-550. https://doi.org/10.1515/tjb-2024-0123
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.urihttps://doi.org/10.1515/tjb-2024-0123
dc.identifier.urihttps://hdl.handle.net/20.500.13055/741
dc.identifier.volume49
dc.identifier.wosWOS:001271127200001
dc.identifier.wosqualityQ4
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynak.otherSCI-E - Science Citation Index Expanded
dc.institutionauthorErkısa Genel, Merve
dc.institutionauthorid0000-0002-3127-742X
dc.language.isoen
dc.publisherWalter De Gruyter
dc.relation.ispartofTurkish Journal Of Biochemistry
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.relation.tubitak223S648
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectOptosis
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
dspace.entity.typePublication

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