List of the scientific projects that received grants

Coordinators:

• EA4034 : Jean-François Goossens
• CHR-Oscar Lambret : Amélie Lansiaux

Mission:

Potentialisation of the activity of topoisomerase I inhibitors by inhibitors of carbonic anhydrase type IX : applications to the treatment of colorectal cancers.

Objectives and rationale:

The limitation of the extracellular acidity using inhibitors of carbonic anhydrase type IX allows better membrane permeation of basic anticancer agents such as the inhibitors of topoisomerase I. This will improve the cytotoxic activity of these compounds. The synthesis and physico-chemical characterization of new carbonic anhydrase IX inhibitors has been successful. This project is done in collaboration with teams from Pr Masereel (University of Namur, Belgium) for molecular modeling and Pr Supuran (University of Florence) for enzymatic assays. The objective of this multidisciplinary project is to develop specific carbonic anhydrase IX inhibitors and to evaluate both in vitro and in vivo the potentialisation of the effects of topoisomerase I inhibitors (derived from campothecin). These compounds will be assayed in colorectal cancer models to achieve this goal.