GSK461364A suppresses proliferation of gastric cancer cells and induces apoptosis

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dc.authoridyulak, fatih/0000-0003-3708-6752
dc.contributor.authorAtaseven, Dilara
dc.contributor.authorTastemur, Seyma
dc.contributor.authorYulak, Fatih
dc.contributor.authorKarabulut, Sebahattin
dc.contributor.authorErgul, Mustafa
dc.date.accessioned2024-10-26T18:07:14Z
dc.date.available2024-10-26T18:07:14Z
dc.date.issued2023
dc.departmentSivas Cumhuriyet Üniversitesi
dc.description.abstractPolo-like kinase 1 (PLK1) is crucial in regulating cell division and has been shown to have an oncogenic function in several cancers. Since PLK1 overexpression is closely related to tumorigenesis and has been correlated with poor clinical outcomes, specific inhibition of PLK1 in cancer cells is a promising approach for developing new anticancer drugs. In this context, the aim of the present study was to evaluated the potential cytotoxic effects of GSK461364A, a competitive inhibitor for PLK1, in gastric cancer cell line SNU-1 cells and explored its cytotoxic mechanism. The cells were exposed to GSK461364A at different concentrations ranging from 1 to 40 mu M for 24 h, and it showed considerable cytotoxicity with an IC50 value of 4.34 mu M. The treatment of SNU-1 cells with GSK461364A results in cell cycle arrest at the G2/M phase, decreased mitochondrial membrane potential, and increased apoptosis as indicated by Annexin V binding assay. In addition, GSK461364A treatment significantly increased the total oxidant (TOS) level, a signal of oxidative stress, and increased cleaved PARP and 8-oxo-dG levels as an indicator of DNA damage. ELISA experiments evaluating Bax, BCL-2, and cleaved caspase 3 also confirmed the apoptotic effect of GSK461364A. Current findings suggest that GSK461364A may be a chemotherapeutic agent in patients with gastric cancer. Nevertheless, more research is needed to evaluate GSK461364A as a cancer treatment drug.
dc.identifier.doi10.1016/j.tiv.2023.105610
dc.identifier.issn0887-2333
dc.identifier.issn1879-3177
dc.identifier.pmid37150268
dc.identifier.scopus2-s2.0-85159313827
dc.identifier.scopusqualityQ2
dc.identifier.urihttps://doi.org/10.1016/j.tiv.2023.105610
dc.identifier.urihttps://hdl.handle.net/20.500.12418/29391
dc.identifier.volume90
dc.identifier.wosWOS:001001404800001
dc.identifier.wosqualityQ3
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.language.isoen
dc.publisherPergamon-Elsevier Science Ltd
dc.relation.ispartofToxicology in Vitro
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.subjectGastric cancer
dc.subjectPLK1 inhibition
dc.subjectGSK461364A
dc.subjectApoptosis
dc.subjectELISA
dc.titleGSK461364A suppresses proliferation of gastric cancer cells and induces apoptosis
dc.typeArticle

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