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Med Sci (Paris). 2015 Mar;31(3):312-9. doi: 10.1051/medsci/20153103017. Epub 2015 Apr 8.

[Chemical libraries dedicated to protein-protein interactions].

[Article in French]

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Molécules thérapeutiques in silico (MTi), université Paris Diderot, Inserm UMR-S973, 35, rue Hélène Brion, 75205 Paris Cedex 13, France.
Centre de recherche en cancérologie de Marseille (CRCM), CNRS UMR7258 ; Inserm U1068 ; institut Paoli-Calmettes ; université d'Aix-Marseille UM105, 27, boulevard Lei Roure,13009, Marseille, France.


The identification of complete networks of protein-protein interactions (PPI) within a cell has contributed to major breakthroughs in understanding biological pathways, host-pathogen interactions and cancer development. As a consequence, PPI have emerged as a new class of promising therapeutic targets. However, they are still considered as a challenging class of targets for drug discovery programs. Recent successes have allowed the characterization of structural and physicochemical properties of protein-protein interfaces leading to a better understanding of how they can be disrupted with small molecule compounds. In addition, characterization of the profiles of PPI inhibitors has allowed the development of PPI-focused libraries. In this review, we present the current efforts at developing chemical libraries dedicated to these innovative targets.

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