Inhibition of Antiestrogen-Promoted Pro-Survival Autophagy and Tamoxifen Resistance in Breast Cancer through Vitamin D Receptor

Nutrients. 2021 May 19;13(5):1715. doi: 10.3390/nu13051715.

Abstract

We determined how vitamin D receptor (VDR) is linked to disease outcome in estrogen receptor-positive (ER+) breast cancer patients treated with tamoxifen (TAM). Breast cancer patients (n = 581) in four different datasets were divided into those expressing higher (above median) and lower levels of VDR in pretreatment ER+ tumors. Across all datasets, TAM-treated patients with higher pretreatment tumor VDR expression exhibited significantly longer recurrence-free survival. Ingenuity pathway analysis identified autophagy and unfolded protein response (UPR) as top differentially expressed pathways between high and low VDR-expressing ER+ cancers. Activation of VDR with vitamin D (VitD), either calcitriol or its synthetic analog EB1089, sensitized MCF-7-derived, antiestrogen-resistant LCC9 human breast cancer cells to TAM, and attenuated increased UPR and pro-survival autophagy. Silencing of VDR blocked these effects through the IRE1α-JNK pathway. Further, silencing of VDR impaired sensitivity to TAM in antiestrogen-responsive LCC1 cells, and prevented the effects of calcitriol and EB1089 on UPR and autophagy. In a preclinical mouse model, dietary VitD supplementation induced VDR activation and reduced carcinogen-induced ER+ mammary tumor incidence. In addition, IRE1α-JNK signaling was downregulated and survival autophagy was inhibited in mammary tumors of VitD-supplemented mice. Thus, activation of VDR is predictive of reduced risk of breast cancer recurrence in ER+ patients, possibly by inhibiting antiestrogen-promoted pro-survival autophagy.

Keywords: autophagy; breast cancer; recurrence-free survival; tamoxifen; vitamin D analogs; vitamin D receptor.

MeSH terms

  • Animals
  • Autophagy / drug effects*
  • Breast / metabolism
  • Breast Neoplasms / drug therapy*
  • Calcitriol / analogs & derivatives
  • Cell Line, Tumor
  • Drug Resistance, Neoplasm / drug effects*
  • Endoribonucleases
  • Estrogen Antagonists / pharmacology
  • Estrogen Receptor Modulators / pharmacology*
  • Estrogen Receptor Modulators / therapeutic use*
  • Female
  • Humans
  • MCF-7 Cells
  • Mice
  • Protein Serine-Threonine Kinases
  • Receptors, Calcitriol / metabolism
  • Tamoxifen / pharmacology*
  • Vitamin D / analogs & derivatives

Substances

  • Estrogen Antagonists
  • Estrogen Receptor Modulators
  • Receptors, Calcitriol
  • VDR protein, human
  • Tamoxifen
  • Vitamin D
  • ERN1 protein, human
  • Protein Serine-Threonine Kinases
  • Endoribonucleases
  • Calcitriol
  • seocalcitol