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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 | 2016-05-23T11:00:34Z | |
dc.date.issued | 2014 | |
dc.identifier.issn | 1860-7187 | |
dc.identifier.uri | https://radar.ibiss.bg.ac.rs/handle/123456789/2215 | |
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.description.sponsorship | Lead Discovery Siena, Srl; Ministry of Education, Science, and Technological Development of Serbia {[}III 41031]; Fundacao para a Ciencia e a Tecnologia (FCT) {[}SFRH/BPD/84634/2012] | |
dc.language | English | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Integrated and Interdisciplinary Research (IIR or III)/41031/RS// | |
dc.relation | Fundação para a Ciência e a Tecnologia (SFRH/BPD/84634/2012) | |
dc.relation | Lead Discovery Siena, Srl | |
dc.relation | COST Action CM1106 (Chemical Approaches to Targeting Drug Resistance in Cancer Stem Cells) | |
dc.rights | restrictedAccess | |
dc.source | Chemmedchem | |
dc.subject | antitumor agents | |
dc.subject | cancer | |
dc.subject | doxorubicin | |
dc.subject | inhibitors | |
dc.subject | multidrug resistance | |
dc.subject | protein-protein interactions | |
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 | |
dc.rights.license | ARR | |
dcterms.abstract | Цау, Yлениа; Вигнароли, Гиулиа; Песиц, Милица; Мори, Маттиа; Ботта, Мауризио; Хилл, Рицхард; Росси, Маттео; Цолеццхиа, Давид; Линк, Wолфганг; Цхиариелло, Марио; Диниц, Јелена; Оттманн, Цхристиан; | |
dc.rights.holder | © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim. | |
dc.citation.issue | 5, SI | |
dc.citation.volume | 9 | |
dc.description.note | Related to: [https://radar.ibiss.bg.ac.rs/handle/123456789/3886]. | |
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 | publishedVersion | en |
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