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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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Bibliografske podrobnosti
Main Authors: 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
Jezik:Inglês
Izdano: 2013
Teme:
Online dostop: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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