Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
8414270 | European Journal of Pharmaceutics and Biopharmaceutics | 2013 | 11 Pages |
Abstract
The aim of this study was to develop clickable prodrugs bearing a tunable pH responsive linker designed for acidic pH-mediated release of histone deacetylase inhibitors. HDACi are an important class of molecules belonging to the epigenetic modulators used for innovative cancer strategies. The behavior of these prodrugs was determined by a bioluminescence resonance energy transfer assay in living tumor cells. This work demonstrated that this innovative type of clickable prodrugs entered cancer cells and showed restored anti proliferative properties attributed to the effective release of the HDAC inhibitors. A correlation between kinetic studies, dose responses, and biological activities was obtained, making such clickable prodrugs good candidates for new strategies in epigenetic-oriented anticancer therapies.
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Authors
Régis Delatouche, Iza Denis, Marion Grinda, Fatima El Bahhaj, Estelle Baucher, Floraine Collette, Valérie Héroguez, Marc Grégoire, Christophe Blanquart, Philippe Bertrand,