Selective inhibitors of mTORC1 activate 4EBP1 and suppress tumor growth

Lee, Bianca J.; Boyer, Jacob A.; Burnett, G. Leslie; Thottumkara, Arun P.; Tibrewal, Nidhi; Wilson, Stacy L.; Hsieh, Tientien; Marquez, Abby; Lorenzana, Edward G.; Evans, James W.; Hulea, Laura; Kiss, Gert; Liu, Hui; Lee, Dong; Larsson, Ola; McLaughlan, Shannon; Topisirovic, Ivan; Wang, Zhengping; Wang, Zhican; Zhao, Yongyuan; Wildes, David; Aggen, James B.; Singh, Mallika; Gill, Adrian L.; Smith, Jacqueline A. M.; Rosen, Neal


Nat Chem Biol 17, 1065–1074 (2021)


This paper highlights the therapeutic promise of mTORC1-selective bi-steric inhibitors in the treatment of tumors driven by the genomic activation of the mTORC1 pathway.  Specifically, the published research details the manner in which these selective inhibitors of mTORC1 potently inhibit tumor growth while causing less toxicity and receptor reactivation, a potential mechanism of adaptive resistance, as compared to conventional mTOR inhibitors.  These study results offer compelling rationale for our recently initiated clinical development program for RMC-5552.

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