Negative regulation of HER2 signaling by the PEST-type protein-tyrosine phosphatase BDP1

J Biol Chem. 2004 Mar 26;279(13):12110-6. doi: 10.1074/jbc.M309527200. Epub 2003 Dec 2.

Abstract

Signaling by receptor tyrosine kinases (RTK) mediates a variety of complex cellular functions and in case of deregulation can contribute to pathophysiological processes. A tight and finely tuned control of RTK activity is therefore critical for the cell. We investigated the role of the PEST-type protein-tyrosine phosphatase BDP1 in the regulation of HER2, a member of the epidermal growth factor receptor (EGFR) family of RTKs. Here we demonstrate that HER2 signaling is highly sensitive to BDP1 activity. Overexpression of BDP1 inhibited ligand-induced activation of HER2 but not that of the closely related EGFR. On the other hand, suppression of endogenous BDP1 expression increased the phosphorylation state of HER2. In addition, BDP1 was able to interfere with downstream signaling events by inhibiting the phosphorylation of the adaptor protein Gab1 and reducing mitogen-activated protein kinase activation. Supported by the finding that BDP1 is coexpressed with HER2 in breast cancer cells, we suggest that BDP1 is an important regulator of HER2 activity and thus the first protein-tyrosine phosphatase shown to be involved in HER2 signal attenuation.

MeSH terms

  • Adaptor Proteins, Signal Transducing
  • Animals
  • Blotting, Western
  • Cell Line
  • Down-Regulation
  • ErbB Receptors / metabolism
  • Gene Expression Regulation, Neoplastic*
  • Genetic Vectors
  • Humans
  • Ligands
  • MAP Kinase Signaling System
  • Mammary Neoplasms, Animal / metabolism
  • Mice
  • Mice, Transgenic
  • Mutation
  • Phosphoproteins / metabolism
  • Phosphorylation
  • Precipitin Tests
  • Protein Binding
  • Protein Tyrosine Phosphatases / metabolism
  • Protein Tyrosine Phosphatases / physiology*
  • Protein Tyrosine Phosphatases, Non-Receptor
  • RNA, Small Interfering / metabolism
  • Receptor, ErbB-2 / biosynthesis*
  • Retroviridae / genetics
  • Signal Transduction*
  • Time Factors
  • Transfection
  • Tumor Suppressor Proteins / physiology

Substances

  • Adaptor Proteins, Signal Transducing
  • GAB1 protein, human
  • Gab1 protein, mouse
  • Ligands
  • Phosphoproteins
  • RNA, Small Interfering
  • Tumor Suppressor Proteins
  • ErbB Receptors
  • Receptor, ErbB-2
  • PTPN18 protein, human
  • Protein Tyrosine Phosphatases
  • Protein Tyrosine Phosphatases, Non-Receptor