Small-molecule ligands bind to a distinct pocket in Ras and inhibit SOS-mediated nucleotide exchange activity

The Ras gene is frequently mutated in cancer, and mutant Ras drives tumorigenesis. Although Ras is a central oncogene, small molecules that bind to Ras in a well-defined manner and exert inhibitory effects have not been uncovered to date. Through an NMR-based fragment screen, we identified a group o...

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Hauptverfasser: Maurer, Till, Garrenton, Lindsay S., Oh, Angela, Pitts, Keith, Anderson, Daniel J., Skelton, Nicholas J., Fauber, Benjamin P., Pan, Borlan, Malek, Shiva, Stokoe, David, Ludlam, Mary J. C., Bowman, Krista K., Wu, Jiansheng, Giannetti, Anthony M., Starovasnik, Melissa A., Mellman, Ira, Jackson, Peter K., Rudolph, Joachim, Wang, Weiru, Fang, Guowei
Format: Artigo
Sprache:Inglês
Veröffentlicht: National Academy of Sciences 2012
Schlagworte:
Biological Sciences
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC3325706/
https://ncbi.nlm.nih.gov/pubmed/22431598
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1073/pnas.1116510109
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