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

1
Human Cancer Biobank Center, University of Ioannina, Ioannina, GR-45110, Greece
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Department of Chemistry, University of Ioannina, Ioannina, GR-45110, Greece
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Department of Materials Science and Engineering, University of Ioannina, Ioannina, GR-45110, Greece
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Institute for Chemistry and Engineering Sciences, 11 Biopolis Way, Helios, #03-08, Singapore 138667, Singapore
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Department of Clinical Hematology,University Hospital of Ioannina, Ioannina, GR-45110, Greece
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Medical School, Oncology Section, University of Ioannina, Ioannina, GR-45110, Greece
*
Authors to whom correspondence should be addressed.
Molecules 2011, 16(6), 4408-4427; https://doi.org/10.3390/molecules16064408
Received: 10 March 2011 / Revised: 4 May 2011 / Accepted: 25 May 2011 / Published: 27 May 2011
(This article belongs to the Special Issue Diversity Oriented Synthesis)
We 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. View Full-Text
Keywords: diversity-oriented synthesis; combinatorial chemistry; protein-protein interactions; cancer diversity-oriented synthesis; combinatorial chemistry; protein-protein interactions; cancer
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Tzakos, A.G.; Fokas, D.; Johannes, C.; Moussis, V.; Hatzimichael, E.; Briasoulis, E. Targeting Oncogenic Protein-Protein Interactions by Diversity Oriented Synthesis and Combinatorial Chemistry Approaches. Molecules 2011, 16, 4408-4427.

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