MNK Inhibition Sensitizes KRAS-Mutant Colorectal Cancer to mTORC1 Inhibition by Reducing eIF4E Phosphorylation and c-MYC Expression

Cancer Discov. 2021 May;11(5):1228-1247. doi: 10.1158/2159-8290.CD-20-0652. Epub 2020 Dec 16.

Abstract

KRAS-mutant colorectal cancers are resistant to therapeutics, presenting a significant problem for ∼40% of cases. Rapalogs, which inhibit mTORC1 and thus protein synthesis, are significantly less potent in KRAS-mutant colorectal cancer. Using Kras-mutant mouse models and mouse- and patient-derived organoids, we demonstrate that KRAS with G12D mutation fundamentally rewires translation to increase both bulk and mRNA-specific translation initiation. This occurs via the MNK/eIF4E pathway culminating in sustained expression of c-MYC. By genetic and small-molecule targeting of this pathway, we acutely sensitize KRASG12D models to rapamycin via suppression of c-MYC. We show that 45% of colorectal cancers have high signaling through mTORC1 and the MNKs, with this signature correlating with a 3.5-year shorter cancer-specific survival in a subset of patients. This work provides a c-MYC-dependent cotargeting strategy with remarkable potency in multiple Kras-mutant mouse models and metastatic human organoids and identifies a patient population that may benefit from its clinical application. SIGNIFICANCE: KRAS mutation and elevated c-MYC are widespread in many tumors but remain predominantly untargetable. We find that mutant KRAS modulates translation, culminating in increased expression of c-MYC. We describe an effective strategy targeting mTORC1 and MNK in KRAS-mutant mouse and human models, pathways that are also commonly co-upregulated in colorectal cancer.This article is highlighted in the In This Issue feature, p. 995.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Colorectal Neoplasms / genetics*
  • Colorectal Neoplasms / metabolism
  • Disease Models, Animal
  • Eukaryotic Initiation Factor-4E / drug effects*
  • Eukaryotic Initiation Factor-4E / metabolism
  • Humans
  • Intracellular Signaling Peptides and Proteins / drug effects*
  • Intracellular Signaling Peptides and Proteins / metabolism
  • MTOR Inhibitors / pharmacology*
  • Mice
  • Mice, Inbred C57BL
  • Phosphorylation
  • Protein Serine-Threonine Kinases / drug effects*
  • Protein Serine-Threonine Kinases / metabolism

Substances

  • Eukaryotic Initiation Factor-4E
  • Intracellular Signaling Peptides and Proteins
  • MTOR Inhibitors
  • MKNK1 protein, human
  • Protein Serine-Threonine Kinases