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SUMMARY:In-cell NMR for real-time studies of protein-ligand interactions i
 n human cells - Dr. Enrico Luchinat\, Department of Agricultural and Food 
 Sciences\, University of Bologna\, and Magnetic Resonance Center (CERM)\, 
 Florence\, Italy
DTSTART:20230607T093000Z
DTEND:20230607T103000Z
UID:TALK202045@talks.cam.ac.uk
CONTACT:114835
DESCRIPTION:In-cell NMR provides insights on biological macromolecules in 
 their native cellular environment at atomic resolution. At CERM\, we have 
 developed an approach for expressing and labelling proteins directly in hu
 man cells\, which is ideally applied to monitor functional processes such 
 as protein folding and maturation\, metal binding\, chemical modifications
 \, and interactions with ligands or with specific partners.(1) The develop
 ment of an NMR bioreactor has made possible to study the above processes i
 n real time. The approach provides insights on intracellular ligand bindin
 g kinetics and thermodynamics\, which are critical to optimize drug penetr
 ance and potency.(2\,3) Recently\, we have developed 19F in-cell NMR metho
 dologies\, which allow protein-observed and ligand-observed screenings on 
 targets that would be otherwise invisible by conventional 1H in-cell NMR.(
 4) Such approaches hold great potential in the development of more effecti
 ve drugs towards pharmacologically relevant targets. \n\n(1) Barbieri\, L.
 \; Luchinat\, E.\; Banci\, L. Characterization of Proteins by In-Cell NMR 
 Spectroscopy in Cultured Mammalian Cells. Nat. Protoc. 2016\, 11 (6)\, 110
 1–1111.\n\n(2) Luchinat\, E.\; Barbieri\, L.\; Cremonini\, M.\; Nocentin
 i\, A.\; Supuran\, C. T.\; Banci\, L. Drug Screening in Human Cells by NMR
  Spectroscopy Allows the Early Assessment of Drug Potency. Angew. Chem. In
 t. Ed. Engl. 2020\, 59 (16)\, 6535–6539. \n\n(3) Luchinat\, E.\; Barbier
 i\, L.\; Cremonini\, M.\; Pennestri\, M.\; Nocentini\, A.\; Supuran\, C. T
 .\; Banci\, L. Determination of Intracellular Protein-Ligand Binding Affin
 ity by Competition Binding in-Cell NMR. Acta Crystallogr. D Struct. Biol. 
 2021\, 77 (Pt 10)\, 1270–1281.\n\n(4) Pham\, L. B. T.\; Costantino\, A.\
 ; Barbieri\, L.\; Calderone\, V.\; Luchinat\, E.\; Banci\, L. Direct Expre
 ssion of Fluorinated Proteins in Human Cells for 19F In-Cell NMR Spectrosc
 opy. J. Am. Chem. Soc. 2023\, 145 (2)\, 1389–1399.\n
LOCATION:Department of Chemistry\, Unilever Lecture Theatre
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