Protein-drug interactions monitored by time-resolved NMR - Enrico Luchinat (University of Florence)

Protein-drug interactions monitored by time-resolved NMR in human cells  

In-cell NMR provides insights on biological macromolecules in their native cellular environment at atomic resolution. At CERM, we developed an approach for expressing and labelling proteins directly in mammalian cells, which is ideally applied to monitor functional processes such protein folding and maturation, chemical modifications, and interactions with ligands or with specific partners. Recently, we applied the methodology to protein-observed ligand screening in living cells, where it can provide critical information on drug penetrance and selectivity, which are related to drug potency. Finally, the development of a bioreactor enabled monitoring the intracellular ligand binding kinetics by real time in-cell NMR.