PRL-1 protein promotes ERK1/2 and RhoA protein activation through a non-canonical interaction with the Src homology 3 domain of p115 Rho GTPase-activating protein

J Biol Chem. 2011 Dec 9;286(49):42316-42324. doi: 10.1074/jbc.M111.286302. Epub 2011 Oct 18.

Abstract

Phosphatases of the regenerating liver (PRL) play oncogenic roles in cancer development and metastasis. Although previous studies indicate that PRL-1 promotes cell growth and migration by activating both the ERK1/2 and RhoA pathways, the mechanism by which it activates these signaling events remains unclear. We have identified a PRL-1-binding peptide (Peptide 1) that shares high sequence identity with a conserved motif in the Src homology 3 (SH3) domain of p115 Rho GTPase-activating protein (GAP). p115 RhoGAP directly binds PRL-1 in vitro and in cells via its SH3 domain. Structural analyses of the PRL-1·Peptide 1 complex revealed a novel protein-protein interaction whereby a sequence motif within the PxxP ligand-binding site of the p115 RhoGAP SH3 domain occupies a folded groove within PRL-1. This prevents the canonical interaction between the SH3 domain of p115 RhoGAP and MEKK1 and results in activation of ERK1/2. Furthermore, PRL-1 binding activates RhoA signaling by inhibiting the catalytic activity of p115 RhoGAP. The results demonstrate that PRL-1 binding to p115 RhoGAP provides a coordinated mechanism underlying ERK1/2 and RhoA activation.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Amino Acid Motifs
  • Animals
  • Cell Cycle Proteins / metabolism*
  • Fibroblasts / metabolism
  • Gene Expression Regulation, Enzymologic*
  • Guanine Nucleotide Exchange Factors / chemistry*
  • HEK293 Cells
  • Humans
  • Immediate-Early Proteins / metabolism*
  • Ligands
  • Membrane Proteins / metabolism*
  • Mice
  • Mitogen-Activated Protein Kinase 1 / metabolism*
  • Mitogen-Activated Protein Kinase 3 / metabolism*
  • Protein Binding
  • Protein Tyrosine Phosphatases / metabolism*
  • Rho Guanine Nucleotide Exchange Factors
  • Signal Transduction
  • rho GTP-Binding Proteins / metabolism
  • src-Family Kinases / metabolism*

Substances

  • Cell Cycle Proteins
  • Guanine Nucleotide Exchange Factors
  • Immediate-Early Proteins
  • Ligands
  • Membrane Proteins
  • Rho Guanine Nucleotide Exchange Factors
  • src-Family Kinases
  • MAPK1 protein, human
  • Mapk1 protein, mouse
  • Mitogen-Activated Protein Kinase 1
  • Mitogen-Activated Protein Kinase 3
  • PTP4A1 protein, human
  • Protein Tyrosine Phosphatases
  • Ptp4a1 protein, mouse
  • rho GTP-Binding Proteins

Associated data

  • PDB/3RZ2