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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Библиографические подробности
Главные авторы: 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
Формат: Artigo
Язык:Inglês
Опубликовано: National Academy of Sciences 2012
Предметы:
Biological Sciences
Online-ссылка: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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