Article
KRAS inhibitors: going noncovalent.
Molecular oncology - 1 Dec 2022
Drosten Matthias, Barbacid Mariano
Abstract excerpt
KRASG12D is the most frequent KRAS mutation in human cancer with particularly high frequencies in pancreatic and colorectal cancer. Informed by the structure of the KRASG12C inhibitor adagrasib, Hallin et al. have now, through multiple rounds of structure-based drug design, identified and validated a potent, selective, and noncovalent KRASG12D inhibitor, MRTX1133. This study demonstrated that MRTX1133 inhibited...
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