Cancer discovery · 2014
A diverse array of cancer-associated MTOR mutations are hyperactivating and can predict rapamycin sensitivity.
СтатьяПоддержка NIH: внешняя программаПоддержка исследования: вне правительства СШАНазвание и аннотация: Перевод пока не подготовлен
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Grabiner Brian C, Nardi Valentina, Birsoy Kıvanc, Possemato Richard, Shen Kuang, Sinha Sumi, Jordan Alexander, Beck Andrew H, Sabatini David M
Аннотация
Genes encoding components of the PI3K-AKT-mTOR signaling axis are frequently mutated in cancer, but few mutations have been characterized in MTOR, the gene encoding the mTOR kinase. Using publicly available tumor genome sequencing data, we generated a comprehensive catalog of mTOR pathway mutations in cancer, identifying 33 MTOR mutations that confer pathway hyperactivation. The mutations cluster in six distinct regions in the C-terminal half of mTOR and occur in multiple cancer types, with one cluster particularly prominent in kidney cancer. The activating mutations do not affect mTOR complex assembly, but a subset reduces binding to the mTOR inhibitor DEPTOR. mTOR complex 1 (mTORC1) signaling in cells expressing various activating mutations remains sensitive to pharmacologic mTOR inhibition, but is partially resistant to nutrient deprivation. Finally, cancer cell lines with hyperactivating MTOR mutations display heightened sensitivity to rapamycin both in culture and in vivo xenografts, suggesting that such mutations confer mTOR pathway dependency.
Предметные рубрики MeSH
AnimalsAntibiotics, AntineoplasticCell Line, TumorDatabases, FactualHEK293 CellsHeLa CellsHumansMAP Kinase Signaling SystemMCF-7 CellsMechanistic Target of Rapamycin Complex 1Mechanistic Target of Rapamycin Complex 2MiceMice, NudeMultiprotein ComplexesMutationNeoplasmsNeoplasms, ExperimentalProtein Kinase InhibitorsSirolimusTOR Serine-Threonine KinasesXenograft Model Antitumor Assays