Survival of pancreatic cancer cells lacking KRAS function

Nat Commun. 2017 Oct 23;8(1):1090. doi: 10.1038/s41467-017-00942-5.

Abstract

Activating mutations in the proto-oncogene KRAS are a hallmark of pancreatic ductal adenocarcinoma (PDAC), an aggressive malignancy with few effective therapeutic options. Despite efforts to develop KRAS-targeted drugs, the absolute dependence of PDAC cells on KRAS remains incompletely understood. Here we model complete KRAS inhibition using CRISPR/Cas-mediated genome editing and demonstrate that KRAS is dispensable in a subset of human and mouse PDAC cells. Remarkably, nearly all KRAS deficient cells exhibit phosphoinositide 3-kinase (PI3K)-dependent mitogen-activated protein kinase (MAPK) signaling and induced sensitivity to PI3K inhibitors. Furthermore, comparison of gene expression profiles of PDAC cells retaining or lacking KRAS reveal a role of KRAS in the suppression of metastasis-related genes. Collectively, these data underscore the potential for PDAC resistance to even the very best KRAS inhibitors and provide insights into mechanisms of response and resistance to KRAS inhibition.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Benzimidazoles / pharmacology
  • Carcinoma, Pancreatic Ductal / genetics
  • Carcinoma, Pancreatic Ductal / metabolism
  • DNA Copy Number Variations / genetics
  • Humans
  • Immunoblotting
  • Indazoles / pharmacology
  • Mice
  • Morpholines / pharmacology
  • Pancreatic Neoplasms / genetics
  • Pancreatic Neoplasms / metabolism*
  • Phenylurea Compounds / pharmacology
  • Piperidines / pharmacology
  • Proto-Oncogene Mas
  • Proto-Oncogene Proteins p21(ras) / genetics
  • Proto-Oncogene Proteins p21(ras) / metabolism*
  • Purines / pharmacology
  • Pyrimidines / pharmacology
  • Pyrimidinones / pharmacology
  • Quinazolinones / pharmacology
  • Sulfonamides / pharmacology
  • Thiazoles / pharmacology

Substances

  • 2-(1H-indazol-4-yl)-6-(4-methanesulfonylpiperazin-1-ylmethyl)-4-morpholin-4-ylthieno(3,2-d)pyrimidine
  • AZD 6244
  • Antineoplastic Agents
  • Benzimidazoles
  • Indazoles
  • MAS1 protein, human
  • Morpholines
  • Phenylurea Compounds
  • Piperidines
  • Proto-Oncogene Mas
  • Purines
  • Pyrimidines
  • Pyrimidinones
  • Quinazolinones
  • Sulfonamides
  • TGX 221
  • Thiazoles
  • Alpelisib
  • (5-(2,4-bis((3S)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol
  • infigratinib
  • Hras protein, mouse
  • Proto-Oncogene Proteins p21(ras)
  • crenolanib
  • idelalisib