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Ligations chimiques : synthèse d'inhibiteurs extracellulaires de la signalisation HGF/SF-MET

Abstract : Use of peptides as biomolecules have been extensively applied to various therapeutic fields (cancer, diabetes, AIDS). The challenge for chemists consists in development of new reliable and efficient strategies. Our work especially focused on the conception of two innovative non native chemical ligations bringing an additionnal asset to the existing state of the art.The first ligation, i.e. thiocarbamate ligation, affords alkylthiocarbamate peptides with remarkable yields. Regarding the second one, the azaGly ligation allows the straightforward synthesis of azaGlypeptides. On the other hand, this thesis deals with the design of new peptides suitable to inhibit the signaling pathway of the tyrosine–kinase MET receptor and its ligand HGF/SF (Hepatocyte Growth factor/Scattor factor). Indeed interfering with MET signaling appears to be a promising therapeutic approach.The thiocarbamate ligation disclosed previously along with a classical thioether ligation have been employed for the chemical library design of sulfonated peptids in order to inhibit extracellular interactions. Binding activities assessment of the chemical libray toward the MET extracellular domain has been achieved using a microarray technology. Biological activities (MTT tests and kinase activity) have also been investigated.
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Submitted on : Tuesday, October 11, 2011 - 10:43:14 AM
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  • HAL Id : tel-00630962, version 1



Soizic Besret. Ligations chimiques : synthèse d'inhibiteurs extracellulaires de la signalisation HGF/SF-MET. Médecine humaine et pathologie. Université du Droit et de la Santé - Lille II, 2011. Français. ⟨NNT : 2011LIL2S003⟩. ⟨tel-00630962⟩



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