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Accueil > Teams > Laboratoire de Chimie Biologique (LCB) > Project ANR F-LAIR : Fluorinated Ligands Approach for the Inhibition of Rotamases

Project ANR F-LAIR : Fluorinated Ligands Approach for the Inhibition of Rotamases

The incorporation of fluorine atoms into biomolecules has gained a considerable interest as they are known to modulate the properties of pharmaceuticals. Fluorine can often favorably and predictably modify their biophysical and chemical properties, such as lipophilicity, chemical and metabolic stability, reactivity and conformation. Fluorinated compounds can also be used as efficient probes for 19F NMR studies. In this project, we plan to take advantage of the properties of the fluorine atoms to develop fluorinated peptides as a new class of inhibitors of Pin1 which is involved in various diseases such as cancer. The introduction of fluorine into peptide substrates should enable (i) the stabilization of the transition state conformation, (ii) a better biological profile, (iii) the study by NMR of the ligand / Pin1 catalytic site interactions and the screening of inhibitors. This project involves a multidisciplinary consortium of chemists expert in organic synthesis, in silico docking studies and biophysical methods such as NMR.