Criblage d'inhibiteurs réversibles et irréversibles des phosphatases CDC25s par spectrométrie de masse - Application à des extraits d'origine végétale

Abstract : The CDC25s phosphatases are key regulators of the physiological cell cycle progression. Their overexpression has been reported in a significant number of cancers and their inhibition appears to be an interesting strategy for treatments. We propose here a rapid screening test allowing the detection of reversible and irreversible CDC25 inhibitors. The test is based on the incubation of the candidate molecules with the human CDC25 proteins followed by an ultrafiltration step. The retentate is then directly analyzed by MALDI-TOFMS to detect reversible inhibitors or submitted to PMF analysis to reveal irreversible inhibitors. In parallel we applied this test to vegetable extracts in order to identify novel CDC25 inhibitors. The CDC25s inhibitory activity of these extracts is also evaluated in vitro thanks to biological tests. It results from this work that one molecule never known for its activity on the CDC25s shows a potential inhibitory effect and is cytotoxic on human cellular lineage
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Estelle Sibille. Criblage d'inhibiteurs réversibles et irréversibles des phosphatases CDC25s par spectrométrie de masse - Application à des extraits d'origine végétale. Autre. Université de Lorraine, 2013. Français. ⟨NNT : 2013LORR0260⟩. ⟨tel-01750541⟩

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