Next Article in Journal
Next Article in Special Issue
Previous Article in Journal
Previous Article in Special Issue
Molecules 2011, 16(6), 4408-4427; doi:10.3390/molecules16064408
Review

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

1,2,* , 3, 4, 2, 5 and 1,5,6,*
Received: 10 March 2011; in revised form: 4 May 2011 / Accepted: 25 May 2011 / Published: 27 May 2011
(This article belongs to the Special Issue Diversity Oriented Synthesis)
Download PDF [501 KB, uploaded 18 June 2014]
Abstract: 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.
Keywords: diversity-oriented synthesis; combinatorial chemistry; protein-protein interactions; cancer diversity-oriented synthesis; combinatorial chemistry; protein-protein interactions; cancer
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Export to BibTeX |
EndNote


MDPI and ACS Style

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.

AMA Style

Tzakos AG, 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(6):4408-4427.

Chicago/Turabian Style

Tzakos, Andreas G.; Fokas, Demosthenes; Johannes, Charlie; Moussis, Vassilios; Hatzimichael, Eleftheria; Briasoulis, Evangelos. 2011. "Targeting Oncogenic Protein-Protein Interactions by Diversity Oriented Synthesis and Combinatorial Chemistry Approaches." Molecules 16, no. 6: 4408-4427.



Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert