Dynamic assembly of the urokinase-type plasminogen activator signaling receptor complex determines the mitogenic activity of urokinase-type plasminogen activator

J Biol Chem. 2005 Apr 29;280(17):17449-57. doi: 10.1074/jbc.M413141200. Epub 2005 Feb 21.

Abstract

The urokinase-type plasminogen activator (uPA) receptor (uPAR) functions in concert with co-receptors, including integrins, FPR-like receptor-1/lipoxin A4 receptor, and the epidermal growth factor receptor (EGFR), to initiate cell signaling. uPAR co-receptors may be dynamically organized into a multiprotein signaling receptor complex. In Chinese hamster ovary-K1 (CHO-K1) cells, uPA-binding to uPAR activates ERK/MAP kinase, even though these cells do not express the EGFR; however, when CHO-K1 cells are transfected to express the EGFR, ERK activation becomes EGFR-dependent. In this study, we demonstrate that ERK activation in response to uPA follows equivalent biphasic kinetics in EGFR-expressing and -deficient CHO-K1 cells. In both cell types, the response is pertussis toxin-sensitive; however, uPA promotes cell proliferation exclusively in the EGFR-expressing cells. uPA-induced mitogenic activity requires activation of both STAT5b and ERK. STAT5b was tyrosine-phosphorylated, in response to uPA, only in EGFR-expressing cells. uPA-induced cell proliferation was blocked by dominant-negative MEK1, dominant-negative STAT5b, and by expression of an EGFR that is mutated at Tyr-845, which is essential for STAT5b activation. In two cell culture models of uPA-stimulated breast cancer growth, MDA-MB 468 cells treated with uPA and MCF-7 cells treated with uPA-plasminogen activator inhibitor-1 complex, proliferation was completely inhibited when EGFR expression or activity was blocked. We conclude that expression and assembly of uPAR co-receptors in a specific cell type determines the response to uPA. The EGFR selectively cooperates with uPAR to mediate mitogenesis.

MeSH terms

  • Animals
  • Bromodeoxyuridine / pharmacology
  • CHO Cells
  • Cell Line, Tumor
  • Cell Proliferation
  • Coloring Agents / pharmacology
  • Cricetinae
  • DNA / metabolism
  • DNA-Binding Proteins / metabolism
  • Enzyme Activation
  • ErbB Receptors / metabolism
  • Extracellular Signal-Regulated MAP Kinases / metabolism
  • Green Fluorescent Proteins / metabolism
  • Humans
  • Immunoprecipitation
  • Kinetics
  • Milk Proteins / metabolism
  • Mutation
  • Pertussis Toxin / pharmacology
  • Phosphorylation
  • Prognosis
  • Protein Binding
  • RNA, Small Interfering / metabolism
  • STAT5 Transcription Factor
  • Signal Transduction*
  • Tetrazolium Salts / pharmacology
  • Thiazoles / pharmacology
  • Time Factors
  • Trans-Activators / metabolism
  • Transfection
  • Tyrosine / metabolism
  • Urokinase-Type Plasminogen Activator / metabolism*
  • src-Family Kinases / metabolism

Substances

  • Coloring Agents
  • DNA-Binding Proteins
  • Milk Proteins
  • RNA, Small Interfering
  • STAT5 Transcription Factor
  • STAT5B protein, human
  • Tetrazolium Salts
  • Thiazoles
  • Trans-Activators
  • Green Fluorescent Proteins
  • Tyrosine
  • DNA
  • Pertussis Toxin
  • ErbB Receptors
  • src-Family Kinases
  • Extracellular Signal-Regulated MAP Kinases
  • Urokinase-Type Plasminogen Activator
  • thiazolyl blue
  • Bromodeoxyuridine