Biochemical screen uncovers small molecules that bind K-Ras and block Sos activation, suggesting a framework for developing targeted cancer therapeutics.
Looking for fragments: A fragment-based screen using NMR spectroscopy was applied to discover ligands that bind to the GTPase K-Ras and modulate the activity of the nucleotide exchange factor Sos. Structural data on how these fragment-derived hits bind to the guanosine diphosphate–K-Ras complex (see picture) provides a starting point for the future discovery of drugs that target K-Ras activation and signaling.
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Sun et al. (2012) studied this question.
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