Article
In situ selectivity profiling and crystal structure of SML-8-73-1, an active site inhibitor of oncogenic K-Ras G12C.
Proceedings of the National Academy of Sciences of the United States of America - 17 Jun 2014
Hunter John C, Gurbani Deepak, Ficarro Scott B, Carrasco Martin A, Lim Sang Min, Choi Hwan Geun, Xie Ting, Marto Jarrod A, Chen Zhe, Gray Nathanael S, Westover Kenneth D
Abstract excerpt
Directly targeting oncogenic V-Ki-ras2 Kirsten rat sarcoma viral oncogene homolog (K-Ras) with small-molecule inhibitors has historically been considered prohibitively challenging. Recent reports of compounds that bind directly to the K-Ras G12C mutant suggest avenues to overcome key obstacles that stand in the way of developing such compounds. We aim to target the guanine nucleotide (GN)-binding pocket because...
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