Interaction between GW2974 and telomeric G-quadruplex DNA: a possible anticancer mechanism
dc.authorid | Elhaty, Ismail A./0000-0003-4492-2181 | |
dc.contributor.author | Elhaty, Ismail A. | |
dc.date.accessioned | 2024-09-11T19:50:29Z | |
dc.date.available | 2024-09-11T19:50:29Z | |
dc.date.issued | 2021 | |
dc.department | İstanbul Gelişim Üniversitesi | en_US |
dc.description.abstract | Human 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.doi | 10.1007/s11696-021-01801-w | |
dc.identifier.endpage | 6333 | en_US |
dc.identifier.issn | 0366-6352 | |
dc.identifier.issn | 2585-7290 | |
dc.identifier.issue | 12 | en_US |
dc.identifier.scopus | 2-s2.0-85111124313 | en_US |
dc.identifier.startpage | 6323 | en_US |
dc.identifier.uri | https://doi.org/10.1007/s11696-021-01801-w | |
dc.identifier.uri | https://hdl.handle.net/11363/7635 | |
dc.identifier.volume | 75 | en_US |
dc.identifier.wos | WOS:000705624700014 | en_US |
dc.identifier.wosquality | Q3 | en_US |
dc.indekslendigikaynak | Web of Science | en_US |
dc.language.iso | en | en_US |
dc.publisher | Springer Int Publ Ag | en_US |
dc.relation.ispartof | Chemical Papers | en_US |
dc.relation.publicationcategory | Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı | en_US |
dc.rights | info:eu-repo/semantics/closedAccess | en_US |
dc.snmz | 20240903_G | en_US |
dc.subject | Telomere | en_US |
dc.subject | Telomerase | en_US |
dc.subject | Quadruplex | en_US |
dc.subject | Cancer | en_US |
dc.subject | GW2974 | en_US |
dc.title | Interaction between GW2974 and telomeric G-quadruplex DNA: a possible anticancer mechanism | en_US |
dc.type | Article | en_US |