Article
Ferrous iron-activatable drug conjugate achieves potent MAPK blockade in KRAS-driven tumors.
The Journal of experimental medicine - 4 Apr 2022
Jiang Honglin, Muir Ryan K, Gonciarz Ryan L, Olshen Adam B, Yeh Iwei, Hann Byron C, Zhao Ning, Wang Yung-Hua, Behr Spencer C, Korkola James E, Evans Michael J, Collisson Eric A, Renslo Adam R
Abstract excerpt
KRAS mutations drive a quarter of cancer mortality, and most are undruggable. Several inhibitors of the MAPK pathway are FDA approved but poorly tolerated at the doses needed to adequately extinguish RAS/RAF/MAPK signaling in the tumor cell. We found that oncogenic KRAS signaling induced ferrous iron (Fe2+) accumulation early in and throughout mutant KRAS-mediated transformation. We converted an FDA-approved MEK...
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