lncRNA MIR100HG-derived miR-100 and miR-125b mediate cetuximab resistance via Wnt/β-catenin signaling

Nat Med. 2017 Nov;23(11):1331-1341. doi: 10.1038/nm.4424. Epub 2017 Oct 16.

Abstract

De novo and acquired resistance, which are largely attributed to genetic alterations, are barriers to effective anti-epidermal-growth-factor-receptor (EGFR) therapy. To generate cetuximab-resistant cells, we exposed cetuximab-sensitive colorectal cancer cells to cetuximab in three-dimensional culture. Using whole-exome sequencing and transcriptional profiling, we found that the long non-coding RNA MIR100HG and two embedded microRNAs, miR-100 and miR-125b, were overexpressed in the absence of known genetic events linked to cetuximab resistance. MIR100HG, miR-100 and miR-125b overexpression was also observed in cetuximab-resistant colorectal cancer and head and neck squamous cell cancer cell lines and in tumors from colorectal cancer patients that progressed on cetuximab. miR-100 and miR-125b coordinately repressed five Wnt/β-catenin negative regulators, resulting in increased Wnt signaling, and Wnt inhibition in cetuximab-resistant cells restored cetuximab responsiveness. Our results describe a double-negative feedback loop between MIR100HG and the transcription factor GATA6, whereby GATA6 represses MIR100HG, but this repression is relieved by miR-125b targeting of GATA6. These findings identify a clinically actionable, epigenetic cause of cetuximab resistance.

MeSH terms

  • Antineoplastic Agents, Immunological / pharmacology*
  • Cell Line, Tumor
  • Cetuximab / pharmacology*
  • Disease Progression
  • Drug Resistance, Neoplasm / genetics*
  • Epigenesis, Genetic
  • GATA6 Transcription Factor / metabolism
  • Humans
  • MicroRNAs / genetics*
  • RNA, Long Noncoding / genetics*
  • Signal Transduction*
  • Wnt Proteins / metabolism
  • beta Catenin / metabolism*

Substances

  • Antineoplastic Agents, Immunological
  • GATA6 Transcription Factor
  • GATA6 protein, human
  • MIRN100 microRNA, human
  • MIRN1260 microRNA, human
  • MicroRNAs
  • RNA, Long Noncoding
  • Wnt Proteins
  • beta Catenin
  • Cetuximab