[PDF][PDF] Genetic dissection of the oncogenic mTOR pathway reveals druggable addiction to translational control via 4EBP-eIF4E

AC Hsieh, M Costa, O Zollo, C Davis, ME Feldman… - Cancer cell, 2010 - cell.com
AC Hsieh, M Costa, O Zollo, C Davis, ME Feldman, JR Testa, O Meyuhas, KM Shokat…
Cancer cell, 2010cell.com
We genetically dissect the contribution of the most prominent downstream translational
components of mTOR signaling toward Akt-driven lymphomagenesis. While phosphorylation
of rpS6 is dispensable for cancer formation, 4EBP-eIF4E exerts significant control over cap-
dependent translation, cell growth, cancer initiation, and progression. This effect is mediated
at least in part through 4EBP-dependent control of Mcl-1 expression, a key antiapoptotic
protein. By using an active site inhibitor of mTOR, PP242, we show a marked therapeutic …
Summary
We genetically dissect the contribution of the most prominent downstream translational components of mTOR signaling toward Akt-driven lymphomagenesis. While phosphorylation of rpS6 is dispensable for cancer formation, 4EBP-eIF4E exerts significant control over cap-dependent translation, cell growth, cancer initiation, and progression. This effect is mediated at least in part through 4EBP-dependent control of Mcl-1 expression, a key antiapoptotic protein. By using an active site inhibitor of mTOR, PP242, we show a marked therapeutic response in rapamycin-resistant tumors. The therapeutic benefit of PP242 is mediated through inhibition of mTORC1-dependent 4EBP-eIF4E hyperactivation. Thus, the 4EBP-eIF4E axis downstream of mTOR is a druggable mediator of translational control and Akt-mediated tumorigenesis that has important implications for the treatment of human cancers.
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