Discovery of Covalent Wild-Type Isocitrate Dehydrogenase 1 (IDH1) Inhibitors Targeting Cys269
A covalent fragment-based approach was used to develop IDH1-C269 selective inhibitors which prevent the key regulatory segment from forming an α-helix required for catalytic competency, and provide structurally validated inhibitors for further development.
Charles P. Brown, Elliot O. Harmer, Ariba Azam et al.
· bioRxiv · 0 citations