Tamoxifen mechanically deactivates hepatic stellate cells via the G protein-coupled estrogen receptor

Oncogene. 2019 Apr;38(16):2910-2922. doi: 10.1038/s41388-018-0631-3. Epub 2018 Dec 21.

Abstract

Tamoxifen has been used for many years to target estrogen receptor signalling in breast cancer cells. Tamoxifen is also an agonist of the G protein-coupled estrogen receptor (GPER), a GPCR ubiquitously expressed in tissues that mediates the acute response to estrogens. Here we report that tamoxifen promotes mechanical quiescence in hepatic stellate cells (HSCs), stromal fibroblast-like cells whose activation triggers and perpetuates liver fibrosis in hepatocellular carcinomas. This mechanical deactivation is mediated by the GPER/RhoA/myosin axis and induces YAP deactivation. We report that tamoxifen decreases the levels of hypoxia-inducible factor-1 alpha (HIF-1α) and the synthesis of extracellular matrix proteins through a mechanical mechanism that involves actomyosin-dependent contractility and mechanosensing of tissue stiffness. Our results implicate GPER-mediated estrogen signalling in the mechanosensory-driven activation of HSCs and put forward estrogenic signalling as an option for mechanical reprogramming of myofibroblast-like cells in the tumour microenvironment. Tamoxifen, with half a century of safe clinical use, might lead this strategy of drug repositioning.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Line
  • Estrogens / metabolism
  • Fibroblasts / drug effects
  • Fibroblasts / metabolism
  • Hepatic Stellate Cells / drug effects*
  • Hepatic Stellate Cells / metabolism*
  • Humans
  • Hypoxia-Inducible Factor 1, alpha Subunit / metabolism
  • Receptors, Estrogen / metabolism*
  • Receptors, G-Protein-Coupled / metabolism*
  • Signal Transduction / drug effects
  • Tamoxifen / pharmacology*
  • Tumor Microenvironment / drug effects

Substances

  • Estrogens
  • GPER1 protein, human
  • Hypoxia-Inducible Factor 1, alpha Subunit
  • Receptors, Estrogen
  • Receptors, G-Protein-Coupled
  • Tamoxifen