Article
Probing the KRas Switch II Groove by Fluorine NMR Spectroscopy.
ACS chemical biology - 21 Oct 2022
Peacock D Matthew, Kelly Mark J S, Shokat Kevan M
Abstract excerpt
While there has been recent success in the development of KRasG12C inhibitors, unmet needs for selective inhibitors of KRasG12D and the remaining oncogenic KRas proteins remain. Here, we applied trifluoromethyl-containing ligands of KRas proteins as competitive probe ligands to assay the occupancy of the switch II pocket by 19F NMR spectroscopy. Structure-activity-relationship studies of probe ligands increased...
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