Interaction between GW2974 and telomeric G-quadruplex DNA: a possible anticancer mechanism

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dc.authoridElhaty, Ismail A./0000-0003-4492-2181
dc.contributor.authorElhaty, Ismail A.
dc.date.accessioned2024-09-11T19:50:29Z
dc.date.available2024-09-11T19:50:29Z
dc.date.issued2021
dc.departmentİstanbul Gelişim Üniversitesien_US
dc.description.abstractHuman telomere consists of tandem repeats of guanines; thus, it can form an intramolecular G-quadruplex structure, which can inhibit the telomerase enzyme that is found active in more than 85% of cancer cells. The present work investigated the interactions of GW2974, a quinazoline derivative with telomeric G-quadruplex AG(3)(TTAGGG)(3.) GW2974 had shown a good affinity to G-quadruplex DNA with a binding constant of 2.41 x 10(6) M-1 and melting temperature shift Delta Tm of 9.9 degrees C. Increasing the GW2974 ratio with DNA up to five times showed an inverse effect on G-quadruplex DNA stability. The stoichiometric ratio between GW2974 and TelQ (per strand) was 2:1. Results obtained from absorption, fluorescence, and CD spectroscopic techniques indicated that GW2974 interacted with G-quadruplex through different binding modes. GW2974 showed good specificity to quadruplex over duplex DNA by 4.71-fold. These results indicated that stabilizing of telomeric G-quadruplex inhibited telomerase enzyme, which could be a potential anticancer mechanism of GW2974.en_US
dc.identifier.doi10.1007/s11696-021-01801-w
dc.identifier.endpage6333en_US
dc.identifier.issn0366-6352
dc.identifier.issn2585-7290
dc.identifier.issue12en_US
dc.identifier.scopus2-s2.0-85111124313en_US
dc.identifier.startpage6323en_US
dc.identifier.urihttps://doi.org/10.1007/s11696-021-01801-w
dc.identifier.urihttps://hdl.handle.net/11363/7635
dc.identifier.volume75en_US
dc.identifier.wosWOS:000705624700014en_US
dc.identifier.wosqualityQ3en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.language.isoenen_US
dc.publisherSpringer Int Publ Agen_US
dc.relation.ispartofChemical Papersen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.snmz20240903_Gen_US
dc.subjectTelomereen_US
dc.subjectTelomeraseen_US
dc.subjectQuadruplexen_US
dc.subjectCanceren_US
dc.subjectGW2974en_US
dc.titleInteraction between GW2974 and telomeric G-quadruplex DNA: a possible anticancer mechanismen_US
dc.typeArticleen_US

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