Clinical Translation of Combined MAPK and Autophagy Inhibition in RAS Mutant Cancer

Int J Mol Sci. 2021 Nov 17;22(22):12402. doi: 10.3390/ijms222212402.

Abstract

RAS (rat sarcoma virus) mutant cancers remain difficult to treat despite the advances in targeted therapy and immunotherapy. Targeted therapies against the components of mitogen-activated protein kinase (MAPK) pathways, including RAS, RAF, MEK, and ERK, have demonstrated activity in BRAF mutant and, in limited cases, RAS mutant cancer. RAS mutant cancers have been found to activate adaptive resistance mechanisms such as autophagy during MAPK inhibition. Here, we review the recent clinically relevant advances in the development of the MAPK pathway and autophagy inhibitors and focus on their application to RAS mutant cancers. We provide analysis of the preclinical rationale for combining the MAPK pathway and autophagy and highlight the most recent clinical trials that have been launched to capitalize on this potentially synthetic lethal approach to cancer therapy.

Keywords: RAS; autophagy; lysosome.

Publication types

  • Review

MeSH terms

  • Animals
  • Autophagy / drug effects*
  • Cell Line, Tumor
  • Drug Resistance, Neoplasm / drug effects
  • Drug Therapy, Combination / methods
  • Extracellular Signal-Regulated MAP Kinases / antagonists & inhibitors*
  • Extracellular Signal-Regulated MAP Kinases / metabolism
  • Humans
  • MAP Kinase Signaling System / drug effects
  • Mutation*
  • Neoplasms / drug therapy*
  • Neoplasms / genetics*
  • Neoplasms / metabolism
  • Neoplasms / pathology
  • Protein Kinase Inhibitors / pharmacology*
  • Protein Kinase Inhibitors / therapeutic use*
  • Protein Processing, Post-Translational / drug effects
  • Proto-Oncogene Proteins B-raf / antagonists & inhibitors
  • Proto-Oncogene Proteins B-raf / metabolism
  • Treatment Outcome
  • ras Proteins / antagonists & inhibitors*
  • ras Proteins / genetics*
  • ras Proteins / metabolism

Substances

  • Protein Kinase Inhibitors
  • Proto-Oncogene Proteins B-raf
  • Extracellular Signal-Regulated MAP Kinases
  • ras Proteins