PHD3 regulates EGFR internalization and signalling in tumours

Nat Commun. 2014 Nov 25:5:5577. doi: 10.1038/ncomms6577.

Abstract

Tumours exploit their hypoxic microenvironment to induce a more aggressive phenotype, while curtailing the growth-inhibitory effects of hypoxia through mechanisms that are poorly understood. The prolyl hydroxylase PHD3 is regulated by hypoxia and plays an important role in tumour progression. Here we identify PHD3 as a central regulator of epidermal growth factor receptor (EGFR) activity through the control of EGFR internalization to restrain tumour growth. PHD3 controls EGFR activity by acting as a scaffolding protein that associates with the endocytic adaptor Eps15 and promotes the internalization of EGFR. In consequence, loss of PHD3 in tumour cells suppresses EGFR internalization and hyperactivates EGFR signalling to enhance cell proliferation and survival. Our findings reveal that PHD3 inactivation provides a novel route of EGFR activation to sustain proliferative signalling in the hypoxic microenvironment.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adaptor Proteins, Vesicular Transport / genetics
  • Adaptor Proteins, Vesicular Transport / metabolism
  • Cell Line, Tumor
  • Cell Proliferation
  • Endocytosis*
  • ErbB Receptors / genetics
  • ErbB Receptors / metabolism*
  • Gene Expression Regulation, Neoplastic
  • Humans
  • Hypoxia-Inducible Factor-Proline Dioxygenases / genetics
  • Hypoxia-Inducible Factor-Proline Dioxygenases / metabolism*
  • Neoplasms / enzymology*
  • Neoplasms / genetics
  • Neoplasms / physiopathology
  • Protein Binding
  • Signal Transduction*

Substances

  • Adaptor Proteins, Vesicular Transport
  • EPN2 protein, human
  • EGLN3 protein, human
  • Hypoxia-Inducible Factor-Proline Dioxygenases
  • EGFR protein, human
  • ErbB Receptors