Irreversible JNK1-JUN inhibition by JNK-IN-8 sensitizes pancreatic cancer to 5-FU/FOLFOX chemotherapy

JCI Insight. 2020 Apr 23;5(8):e129905. doi: 10.1172/jci.insight.129905.

Abstract

Over 55,000 people in the United States are diagnosed with pancreatic ductal adenocarcinoma (PDAC) yearly, and fewer than 20% of these patients survive a year beyond diagnosis. Chemotherapies are considered or used in nearly every PDAC case, but there is limited understanding of the complex signaling responses underlying resistance to these common treatments. Here, we take an unbiased approach to study protein kinase network changes following chemotherapies in patient-derived xenograft (PDX) models of PDAC to facilitate design of rational drug combinations. Proteomics profiling following chemotherapy regimens reveals that activation of JNK-JUN signaling occurs after 5-fluorouracil plus leucovorin (5-FU + LEU) and FOLFOX (5-FU + LEU plus oxaliplatin [OX]), but not after OX alone or gemcitabine. Cell and tumor growth assays with the irreversible inhibitor JNK-IN-8 and genetic manipulations demonstrate that JNK and JUN each contribute to chemoresistance and cancer cell survival after FOLFOX. Active JNK1 and JUN are specifically implicated in these effects, and synergy with JNK-IN-8 is linked to FOLFOX-mediated JUN activation, cell cycle dysregulation, and DNA damage response. This study highlights the potential for JNK-IN-8 as a biological tool and potential combination therapy with FOLFOX in PDAC and reinforces the need to tailor treatment to functional characteristics of individual tumors.

Keywords: Cancer; Cell stress; Oncology; Protein kinases; Therapeutics.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Combined Chemotherapy Protocols
  • Carcinoma, Pancreatic Ductal*
  • Drug Evaluation, Preclinical
  • Drug Resistance, Neoplasm / drug effects*
  • Fluorouracil / pharmacology
  • Humans
  • Leucovorin
  • MAP Kinase Kinase 4 / antagonists & inhibitors
  • Mice
  • Mitogen-Activated Protein Kinase 8 / antagonists & inhibitors
  • Organoplatinum Compounds
  • Pancreatic Neoplasms*
  • Xenograft Model Antitumor Assays

Substances

  • Antineoplastic Agents
  • Organoplatinum Compounds
  • Mitogen-Activated Protein Kinase 8
  • MAP Kinase Kinase 4
  • Leucovorin
  • Fluorouracil

Supplementary concepts

  • Folfox protocol