A Wnt-Independent LGR4-EGFR Signaling Axis in Cancer Metastasis

Cancer Res. 2021 Sep 1;81(17):4441-4454. doi: 10.1158/0008-5472.CAN-21-1112. Epub 2021 Jun 7.

Abstract

Leucine-rich repeat-containing G protein-coupled receptors 4, 5, and 6 (LGR4/5/6) play critical roles in development and cancer. The widely accepted mechanism is that these proteins, together with their R-spondin ligands, stabilize Wnt receptors, thus potentiating Wnt signaling. Here we show that LGR4 enhanced breast cancer cell metastasis even when Wnt signaling was deactivated pharmacologically or genetically. Furthermore, LGR4 mutants that cannot potentiate Wnt signaling nevertheless promoted breast cancer cell migration and invasion in vitro and breast cancer metastasis in vivo. Multiomic screening identified EGFR as a crucial mediator of LGR4 activity in cancer progression. Mechanistically, LGR4 interacted with EGFR and blocked EGFR ubiquitination and degradation, resulting in persistent EGFR activation. Together, these data uncover a Wnt-independent LGR4-EGFR signaling axis with broad implications for cancer progression and targeted therapy. SIGNIFICANCE: This work demonstrates a Wnt-independent mechanism by which LGR4 promotes cancer metastasis.See related commentary by Stevens and Williams, p. 4397.

Publication types

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

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Cell Movement
  • Disease Progression
  • ErbB Receptors / metabolism*
  • Female
  • HEK293 Cells
  • Humans
  • In Vitro Techniques
  • Kaplan-Meier Estimate
  • Mice
  • Mice, Nude
  • Neoplasm Invasiveness
  • Neoplasm Metastasis*
  • Neoplasm Transplantation
  • Proteome / metabolism
  • Receptors, G-Protein-Coupled / metabolism*
  • Signal Transduction*
  • Tissue Array Analysis
  • Ubiquitin / metabolism
  • Wnt Proteins / metabolism*
  • Wnt Signaling Pathway

Substances

  • LGR4 protein, human
  • Proteome
  • Receptors, G-Protein-Coupled
  • Ubiquitin
  • Wnt Proteins
  • ErbB Receptors