Article
Biostructural, biochemical and biophysical studies of mutant IDH1.
Nature communications - 9 Sept 2024
McCoy Mark A, Lu Jun, Richard Miller F, Soisson Stephen M, Lam Michael H, Fischer Christian
Abstract excerpt
We report bio-structural, bio-chemical and bio-physical evidence demonstrating how small molecules can bind to both wild-type and mutant IDH1, but only inhibit the enzymatic activity of the mutant isoform. Enabled through x-ray crystallography, we characterized a series of small molecule inhibitors that bound to mutant IDH1 differently than the marketed inhibitor Ivosidenib, for which we have determined the x-ray...
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