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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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Wedi'i Gadw mewn:
Manylion Llyfryddiaeth
Prif Awduron: 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.
Fformat: Artigo
Iaith:Inglês
Cyhoeddwyd: 2013
Pynciau:
Mynediad Ar-lein: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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