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Discovery of 14‐3‐3 Protein–Protein Interaction Inhibitors that Sensitize Multidrug‐Resistant Cancer Cells to Doxorubicin and the Akt Inhibitor GSK690693
dc.creator | Mori, Mattia | |
dc.creator | Vignaroli, Giulia | |
dc.creator | Cau, Ylenia | |
dc.creator | Dinić, Jelena | |
dc.creator | Hill, Richard | |
dc.creator | Rossi, Matteo | |
dc.creator | Colecchia, David | |
dc.creator | Pešić, Milica | |
dc.creator | Link, Wolfgang | |
dc.creator | Chiariello, Mario | |
dc.creator | Ottmann, Christian | |
dc.creator | Botta, Maurizio | |
dc.date.accessioned | 2020-09-18T11:59:58Z | |
dc.date.available | 2015-04-08 | |
dc.date.issued | 2014 | |
dc.identifier.issn | 1860-7187 | |
dc.identifier.uri | https://chemistry-europe.onlinelibrary.wiley.com/doi/full/10.1002/cmdc.201400044 | |
dc.identifier.uri | https://radar.ibiss.bg.ac.rs/123456789/3886 | |
dc.description.abstract | 14-3-3 is a family of highly conserved adapter proteins that is attracting much interest among medicinal chemists. Small-molecule inhibitors of 14-3-3 protein-protein interactions (PPIs) are in high demand, both as tools to increase our understanding of 14-3-3 actions in human diseases and as leads to develop innovative therapeutic agents. Herein we present the discovery of novel 14-3-3 PPI inhibitors through a multidisciplinary strategy combining molecular modeling, organic synthesis, image-based high-content analysis of reporter cells, and in vitro assays using cancer cells. Notably, the two most active compounds promoted the translocation of c-Abl and FOXO pro-apoptotic factors into the nucleus and sensitized multidrug-resistant cancer cells to apoptotic inducers such as doxorubicin and the pan-Akt inhibitor GSK690693, thus becoming valuable lead candidates for further optimization. Our results emphasize the possible role of 14-3-3 PPI inhibitors in anticancer combination therapies. | en |
dc.language.iso | en | sr |
dc.publisher | Weinheim : Wiley-VCH | sr |
dc.relation | info:eu-repo/grantAgreement/MESTD/Integrated and Interdisciplinary Research (IIR or III)/41031/RS// | sr |
dc.relation | Fundação para a Ciência e a Tecnologia (SFRH/BPD/84634/2012) | sr |
dc.relation | Lead Discovery Siena, Srl | sr |
dc.relation | COST Action CM1106 (Chemical Approaches to Targeting Drug Resistance in Cancer Stem Cells) | sr |
dc.rights | embargoedAccess | sr |
dc.source | ChemMedChem | sr |
dc.subject | antitumor agents | sr |
dc.subject | cancer | sr |
dc.subject | doxorubicin | sr |
dc.subject | inhibitors | sr |
dc.subject | multidrug resistance | sr |
dc.subject | protein-protein interactions | sr |
dc.title | Discovery of 14‐3‐3 Protein–Protein Interaction Inhibitors that Sensitize Multidrug‐Resistant Cancer Cells to Doxorubicin and the Akt Inhibitor GSK690693 | en |
dc.type | article | sr |
dc.rights.license | ARR | sr |
dc.rights.holder | © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim. | sr |
dc.citation.issue | 5 | |
dc.citation.volume | 9 | |
dc.description.note | This is the peer-reviewed version of the following article: Mori M, Vignaroli G, Cau Y, et al. Discovery of 14-3-3 protein-protein interaction inhibitors that sensitize multidrug-resistant cancer cells to doxorubicin and the Akt inhibitor GSK690693. ChemMedChem. 2014;9(5):973-983. doi:10.1002/ cmdc.201400044, which has been published in final form at [https:// doi.org/10.1002/cmdc.201400044]. This article may be used for non- commercial purposes in accordance with Wiley-VCH Terms and Conditions for Self-Archiving. | |
dc.description.note | Related to: [https://radar.ibiss.bg.ac.rs/handle/123456789/2215]. | |
dc.identifier.doi | 10.1002/cmdc.201400044 | |
dc.identifier.pmid | 24715717 | |
dc.identifier.scopus | 2-s2.0-84899975034 | |
dc.identifier.wos | 000335001700012 | |
dc.citation.spage | 973 | |
dc.citation.epage | 983 | |
dc.type.version | acceptedVersion | sr |
dc.identifier.fulltext | https://radar.ibiss.bg.ac.rs/bitstream/id/7333/10.1002cmdc.201400044.pdf |