The thyroid hormone-αvβ3 integrin axis in ovarian cancer: regulation of gene transcription and MAPK-dependent proliferation

Oncogene. 2016 Apr 14;35(15):1977-87. doi: 10.1038/onc.2015.262. Epub 2015 Jul 13.

Abstract

Ovarian carcinoma is the fifth common cause of cancer death in women, despite advanced therapeutic approaches. αvβ3 integrin, a plasma membrane receptor, binds thyroid hormones (L-thyroxine, T4; 3,5,3'-triiodo-L-thyronine, T3) and is overexpressed in ovarian cancer. We have demonstrated selective binding of fluorescently labeled hormones to αvβ3-positive ovarian cancer cells but not to integrin-negative cells. Physiologically relevant T3 (1 nM) and T4 (100 nM) concentrations in OVCAR-3 (high αvβ3) and A2780 (low αvβ3) cells promoted αv and β3 transcription in association with basal integrin levels. This transcription was effectively blocked by RGD (Arg-Gly-Asp) peptide and neutralizing αvβ3 antibodies, excluding T3-induced β3 messenger RNA, suggesting subspecialization of T3 and T4 binding to the integrin receptor pocket. We have provided support for extracellular regulated kinase (ERK)-mediated transcriptional regulation of the αv monomer by T3 and of β3 monomer by both hormones and documented a rapid (30-120 min) and dose-dependent (0.1-1000 nM) ERK activation. OVCAR-3 cells and αvβ3-deficient HEK293 cells treated with αvβ3 blockers confirmed the requirement for an intact thyroid hormone-integrin interaction in ERK activation. In addition, novel data indicated that T4, but not T3, controls integrin's outside-in signaling by phosphorylating tyrosine 759 in the β3 subunit. Both hormones induced cell proliferation (cell counts), survival (Annexin-PI), viability (WST-1) and significantly reduced the expression of genes that inhibit cell cycle (p21, p16), promote mitochondrial apoptosis (Nix, PUMA) and tumor suppression (GDF-15, IGFBP-6), particularly in cells with high integrin expression. At last, we have confirmed that hypothyroid environment attenuated ovarian cancer growth using a novel experimental platform that exploited paired euthyroid and severe hypothyroid serum samples from human subjects. To conclude, our data define a critical role for thyroid hormones as potent αvβ3-ligands, driving ovarian cancer cell proliferation and suggest that disruption of this axis may present a novel treatment strategy in this aggressive disease.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antibodies, Neutralizing / pharmacology
  • Cell Division / drug effects
  • Cell Line, Tumor
  • Culture Media / pharmacology
  • Enzyme Activation
  • Extracellular Signal-Regulated MAP Kinases / metabolism
  • Female
  • Gene Expression Regulation, Neoplastic / drug effects
  • Humans
  • Hypothyroidism / blood
  • Integrin alphaV / genetics
  • Integrin alphaV / metabolism
  • Integrin alphaVbeta3 / biosynthesis
  • Integrin alphaVbeta3 / genetics
  • Integrin alphaVbeta3 / immunology
  • Integrin alphaVbeta3 / physiology*
  • Integrin beta3 / genetics
  • Integrin beta3 / metabolism
  • MAP Kinase Signaling System / drug effects
  • MAP Kinase Signaling System / physiology*
  • Neoplasm Proteins / biosynthesis
  • Neoplasm Proteins / genetics
  • Neoplasm Proteins / physiology*
  • Neoplasms, Hormone-Dependent / genetics
  • Neoplasms, Hormone-Dependent / metabolism*
  • Neoplasms, Hormone-Dependent / pathology
  • Oligopeptides / pharmacology
  • Ovarian Neoplasms / genetics
  • Ovarian Neoplasms / metabolism*
  • Ovarian Neoplasms / pathology
  • Phosphorylation
  • Protein Processing, Post-Translational
  • RNA, Messenger / biosynthesis
  • RNA, Neoplasm / biosynthesis
  • Thyroxine / blood
  • Thyroxine / pharmacology
  • Thyroxine / physiology*
  • Transcription, Genetic / drug effects
  • Transcription, Genetic / physiology
  • Triiodothyronine / blood
  • Triiodothyronine / pharmacology
  • Triiodothyronine / physiology*

Substances

  • Antibodies, Neutralizing
  • Culture Media
  • Integrin alphaV
  • Integrin alphaVbeta3
  • Integrin beta3
  • Neoplasm Proteins
  • Oligopeptides
  • RNA, Messenger
  • RNA, Neoplasm
  • Triiodothyronine
  • arginyl-glycyl-aspartic acid
  • Extracellular Signal-Regulated MAP Kinases
  • Thyroxine