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A New Strategy for Glioblastoma Treatment: In Vitro and In Vivo Preclinical Characterization of Si306, a Pyrazolo[3,4-d]Pyrimidine Dual Src/P-Glycoprotein Inhibitor
dc.creator | Fallacara, Ana Lucia | |
dc.creator | Zamperini, Claudio | |
dc.creator | Podolski-Renić, Ana | |
dc.creator | Dinić, Jelena | |
dc.creator | Stanković, Tijana | |
dc.creator | Nešović, Marija | |
dc.creator | Mancini, Arianna | |
dc.creator | Rango, Enrico | |
dc.creator | Iovenitti, Giulia | |
dc.creator | Molinari, Alessio | |
dc.creator | Bugli, Francesca | |
dc.creator | Sanguinetti, Maurizio | |
dc.creator | Torelli, Riccardo | |
dc.creator | Martini, Maurizio | |
dc.creator | Maccari, Laura | |
dc.creator | Valoti, Massimo | |
dc.creator | Dreassi, Elena | |
dc.creator | Botta, Maurizio | |
dc.creator | Pešić, Milica | |
dc.creator | Schenone, Silvia | |
dc.date.accessioned | 2019-07-04T12:30:21Z | |
dc.date.available | 2019-07-04T12:30:21Z | |
dc.date.issued | 2019 | |
dc.identifier.issn | 2072-6694 | |
dc.identifier.uri | https://www.mdpi.com/2072-6694/11/6/848 | |
dc.identifier.uri | https://radar.ibiss.bg.ac.rs/handle/123456789/3379 | |
dc.description.abstract | Overexpression of P-glycoprotein (P-gp) and other ATP-binding cassette (ABC) transporters in multidrug resistant (MDR) cancer cells is responsible for the reduction of intracellular drug accumulation, thus decreasing the efficacy of chemotherapeutics. P-gp is also found at endothelial cells’ membrane of the blood-brain barrier, where it limits drug delivery to central nervous system (CNS) tumors. We have previously developed a set of pyrazolo[3,4-d]pyrimidines and their prodrugs as novel Src tyrosine kinase inhibitors (TKIs), showing a significant activity against CNS tumors in in vivo. Here we investigated the interaction of the most promising pair of drug/prodrug with P-gp at the cellular level. The tested compounds were found to increase the intracellular accumulation of Rho 123, and to enhance the efficacy of paclitaxel in P-gp overexpressing cells. Encouraging pharmacokinetics properties and tolerability in vivo were also observed. Our findings revealed a novel role of pyrazolo[3,4-d]pyrimidines which may be useful for developing a new effective therapy in MDR cancer treatment, particularly against glioblastoma. | en |
dc.language.iso | en | sr |
dc.relation | info:eu-repo/grantAgreement/MESTD/Integrated and Interdisciplinary Research (IIR or III)/41031/RS// | sr |
dc.relation | COST Actions CM1106—Chemical Approaches to Targeting Drug Resistance in Cancer Stem Cells | sr |
dc.relation | COST Action CM1407—Challenging organic syntheses inspired by nature—from natural products chemistry to drug discovery | sr |
dc.relation | AIRC (Associazione Italiana per la Ricerca sul Cancro) Grant IG-2015, code 17677 | sr |
dc.rights | openAccess | sr |
dc.rights.uri | https://creativecommons.org/licenses/by/4.0/ | |
dc.source | Cancers | sr |
dc.subject | Glioblastoma | sr |
dc.subject | Multidrug resistance | sr |
dc.subject | P-gp inhibitors | sr |
dc.subject | Src inhibitors | sr |
dc.subject | In vitro ADME | sr |
dc.subject | Pharmacokinetics | sr |
dc.subject | Brain distribution | sr |
dc.subject | Tolerability | sr |
dc.title | A New Strategy for Glioblastoma Treatment: In Vitro and In Vivo Preclinical Characterization of Si306, a Pyrazolo[3,4-d]Pyrimidine Dual Src/P-Glycoprotein Inhibitor | en |
dc.type | article | sr |
dc.rights.license | BY | sr |
dc.rights.holder | © 2019 by the authors | sr |
dc.citation.issue | 6 | |
dc.citation.volume | 11 | |
dc.identifier.doi | 10.3390/cancers11060848 | |
dc.identifier.pmid | 31248184 | |
dc.identifier.scopus | 2-s2.0-85071177551 | |
dc.identifier.wos | 000475351200112 | |
dc.citation.apa | Fallacara, A. L., Zamperini, C., Podolski-Renić, A., Dinić, J., Stanković, T., Stepanović, M., et al. (2019). A New Strategy for Glioblastoma Treatment: In Vitro and In Vivo Preclinical Characterization of Si306, a Pyrazolo[3,4-d]Pyrimidine Dual Src/P-Glycoprotein Inhibitor. Cancers, 11(6), 848. | |
dc.citation.vancouver | Fallacara AL, Zamperini C, Podolski-Renić A, Dinić J, Stanković T, Stepanović M, Mancini A, Rango E, Iovenitti G, Molinari A, Bugli F, Sanguinetti M, Torelli R, Martini M, Maccari L, Valoti M, Dreassi E, Botta M, Pešić M, Schenone S. A New Strategy for Glioblastoma Treatment: In Vitro and In Vivo Preclinical Characterization of Si306, a Pyrazolo[3,4-d]Pyrimidine Dual Src/P-Glycoprotein Inhibitor. Cancers (Basel). 2019;11(6):848. | |
dc.citation.spage | 848 | |
dc.type.version | publishedVersion | sr |
dc.identifier.fulltext | https://radar.ibiss.bg.ac.rs/bitstream/id/5112/bitstream_5112.pdf | |
dc.citation.rank | M21 |