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Synthelis and Horiba

Validation of the activity of G-protein-coupled receptors (GPCRs) using SPRi

 

Case study using functional CxCR4

 

G-protein-coupled receptors (GPCRs) are among the best therapeutic targets for a wide spectrum of diseases, including cancer and immunode!ciency disorders. However, they are underused in clinic, the production of su"cient amounts of functional proteins with conserved conformation, still remaining a challenge. Here we present a series of experiments realized with functional CxCR4-containing proteoliposomes produced by SYNTHELIS, using a patented cell-free system, to study the interaction with clinically relevant ligands, such as SDF1-#, T22 and AMD 3100. We demonstrate the interest of the SPRi technology (HORIBA Scienti!c) for the determination of GPCR-ligand interactions, independently of the binding site. These results con!rm the usefulness of SPRi as a technique to carry out primary screenings and to obtain relevant pharmacokinetic data.

 

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