Targeting Oncogenic Protein-Protein Interactions by Diversity Oriented Synthesis and Combinatorial Chemistry Approaches

dc.contributor.authorTzakos, A. G.en
dc.contributor.authorFokas, D.en
dc.contributor.authorJohannes, C.en
dc.contributor.authorMoussis, V.en
dc.contributor.authorHatzimichael, E.en
dc.contributor.authorBriasoulis, E.en
dc.date.accessioned2015-11-24T16:49:58Z
dc.date.available2015-11-24T16:49:58Z
dc.identifier.issn1420-3049-
dc.identifier.urihttps://olympias.lib.uoi.gr/jspui/handle/123456789/9551
dc.rightsDefault Licence-
dc.subjectdiversity-oriented synthesisen
dc.subjectcombinatorial chemistryen
dc.subjectprotein-protein interactionsen
dc.subjectcanceren
dc.subjectsmall-molecule antagonistsen
dc.subjectbcl-2 family proteinsen
dc.subjectcancer-therapyen
dc.subjectc-mycen
dc.subjectnatural-productsen
dc.subjectdrug discoveryen
dc.subjectp53 pathwayen
dc.subjectepigenetic therapyen
dc.subjectbreast-canceren
dc.subjectinhibitorsen
dc.titleTargeting Oncogenic Protein-Protein Interactions by Diversity Oriented Synthesis and Combinatorial Chemistry Approachesen
heal.abstractWe are currently witnessing a decline in the development of efficient new anticancer drugs, despite the salient efforts made on all fronts of cancer drug discovery. This trend presumably relates to the substantial heterogeneity and the inherent biological complexity of cancer, which hinder drug development success. Protein-protein interactions (PPIs) are key players in numerous cellular processes and aberrant interruption of this complex network provides a basis for various disease states, including cancer. Thus, it is now believed that cancer drug discovery, in addition to the design of single-targeted bioactive compounds, should also incorporate diversity-oriented synthesis (DOS) and other combinatorial strategies in order to exploit the ability of multi-functional scaffolds to modulate multiple protein-protein interactions (biological hubs). Throughout the review, we highlight the chemistry driven approaches to access diversity space for the discovery of small molecules that disrupt oncogenic PPIs, namely the p53-Mdm2, Bcl-2/Bcl-xL-BH3, Myc-Max, and p53-Mdmx/Mdm2 interactions.en
heal.accesscampus-
heal.fullTextAvailabilityTRUE-
heal.identifier.primaryDOI 10.3390/molecules16064408-
heal.identifier.secondary<Go to ISI>://000292032700009-
heal.identifier.secondaryhttp://www.mdpi.com/1420-3049/16/6/4408/pdf-
heal.journalNameMoleculesen
heal.journalTypepeer reviewed-
heal.languageen-
heal.publicationDate2011-
heal.recordProviderΠανεπιστήμιο Ιωαννίνων. Σχολή Θετικών Επιστημών. Τμήμα Χημείαςel
heal.typejournalArticle-
heal.type.elΆρθρο Περιοδικούel
heal.type.enJournal articleen

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