Therapeutic Targeting of Oncogenic K-Ras by a Covalent Catalytic Site Inhibitor

[Image: see text] We report the synthesis of a GDP analogue, SML-8-73-1, and a prodrug derivative, SML-10-70-1, which are selective, direct-acting covalent inhibitors of the K-Ras G12C mutant relative to wild-type Ras. Biochemical and biophysical measurements suggest that modification of K-Ras with...

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Auteurs principaux: Lim, Sang Min, Westover, Kenneth D., Ficarro, Scott B., Harrison, Rane A., Choi, Hwan Geun, Pacold, Michael E., Carrasco, Martin, Hunter, John, Kim, Nam Doo, Xie, Ting, Sim, Taebo, Jänne, Pasi A., Meyerson, Matthew, Marto, Jarrod A., Engen, John R., Gray, Nathanael S.
Format: Artigo
Langue:Inglês
Publié: 2013
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Article
Accès en ligne:https://ncbi.nlm.nih.gov/pmc/articles/PMC3914205/
https://ncbi.nlm.nih.gov/pubmed/24259466
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1002/anie.201307387
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