EGFR-Targeted Pentacyclic Triterpene Analogues for Glioma Therapy

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dc.authoridRadwan, Mohamed Osman/0000-0002-9220-2659
dc.authoridEMİRDAĞ, SAFİYE/0000-0002-1676-2881
dc.authoridAltıntop, Mehlika Dilek/0000-0002-8159-663X
dc.authoridSever, Belgin/0000-0003-4847-9711
dc.authoridCiftci, Halilibrahim/0000-0002-9796-7669
dc.authoridULUSOY, NAFIA GOKCE/0000-0001-6604-7838
dc.authorscopusid56624185800
dc.authorscopusid55797332300
dc.authorscopusid56789933000
dc.authorscopusid57221807220
dc.authorscopusid6503914739
dc.authorscopusid57211138682
dc.authorscopusid57211135955
dc.authorwosidRadwan, Mohamed Osman/AAX-3535-2021
dc.authorwosidEMİRDAĞ, SAFİYE/T-7524-2018
dc.authorwosidSever, Belgin/V-8319-2017
dc.authorwosidAltıntop, Mehlika Dilek/J-4787-2019
dc.contributor.authorCiftci, Halil I.
dc.contributor.authorRadwan, Mohamed O.
dc.contributor.authorSever, Belgin
dc.contributor.authorHamdy, Ahmed K.
dc.contributor.authorEmirdag, Safiye
dc.contributor.authorUlusoy, N. Gokce
dc.contributor.authorSozer, Ece
dc.date.accessioned2023-01-12T20:15:36Z
dc.date.available2023-01-12T20:15:36Z
dc.date.issued2021
dc.departmentN/A/Departmenten_US
dc.description.abstractGlioma, particularly its most malignant form, glioblastoma multiforme (GBM), is the most common and aggressive malignant central nervous system tumor. The drawbacks of the current chemotherapy for GBM have aroused curiosity in the search for targeted therapies. Aberrantly overexpressed epidermal growth factor receptor (EGFR) in GBM results in poor prognosis, low survival rates, poor responses to therapy and recurrence, and therefore EGFR-targeted therapy stands out as a promising approach for the treatment of gliomas. In this context, a series of pentacyclic triterpene analogues were subjected to in vitro and in silico assays, which were conducted to assess their potency as EGFR-targeted anti-glioma agents. In particular, compound 10 was the most potent anti-glioma agent with an IC50 value of 5.82 mu M towards U251 human glioblastoma cells. Taking into account its low cytotoxicity to peripheral blood mononuclear cells (PBMCs), compound 10 exerts selective antitumor action towards Jurkat human leukemic T-cells. This compound also induced apoptosis and inhibited EGFR with an IC50 value of 9.43 mu M compared to erlotinib (IC50 = 0.06 mu M). Based on in vitro and in silico data, compound 10 stands out as a potential orally bioavailable EGFR-targeted anti-glioma agent endowed with the ability to cross the blood-brain barrier (BBB).en_US
dc.description.sponsorshipAnadolu University Scientific Research Projects Commission [1902S013]; Bilateral Joint Research Project from the Japanese Society for the Promotion of Science [18039111-000102]en_US
dc.description.sponsorshipThis research was funded by Anadolu University Scientific Research Projects Commission, grant number 1902S013. M.F. acknowledges support by Bilateral Joint Research Project from the Japanese Society for the Promotion of Science (the grant no: 18039111-000102).en_US
dc.identifier.doi10.3390/ijms222010945
dc.identifier.issn1422-0067
dc.identifier.issue20en_US
dc.identifier.pmid34681605en_US
dc.identifier.scopus2-s2.0-85116748721en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.urihttps://doi.org/10.3390/ijms222010945
dc.identifier.urihttps://hdl.handle.net/11454/78522
dc.identifier.volume22en_US
dc.identifier.wosWOS:000713117400001en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherMdpien_US
dc.relation.ispartofInternational Journal of Molecular Sciencesen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.subjectapoptosisen_US
dc.subjectepidermal growth factor receptoren_US
dc.subjectglioblastoma multiformeen_US
dc.subjectgliomasen_US
dc.subjectpentacyclic triterpenesen_US
dc.subjectmolecular dockingen_US
dc.subjectDerivativesen_US
dc.subjectAciden_US
dc.subjectGlioblastomaen_US
dc.subjectAnticanceren_US
dc.subjectMechanismsen_US
dc.subjectBetulinen_US
dc.subjectKinaseen_US
dc.titleEGFR-Targeted Pentacyclic Triterpene Analogues for Glioma Therapyen_US
dc.typeArticleen_US

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