Prolactin inhibits activity of pyruvate kinase M2 to stimulate cell proliferation

Mol Endocrinol. 2010 Dec;24(12):2356-65. doi: 10.1210/me.2010-0219. Epub 2010 Oct 20.

Abstract

Mitogenic and prosurvival effects underlie the tumorigenic roles of prolactin (PRL) in the pathogenesis of breast cancer. PRL signaling is mediated through its receptor (PRLr). A proteomics screen identified the pyruvate kinase M2 (PKM2), a glycolytic enzyme known to play an important role in tumorigenesis, as a protein that constitutively interacts with PRLr. Treatment of cells with PRL inhibited pyruvate kinase activity and increased the lactate content in human cells in a manner that was dependent on the abundance of PRLr, activation of Janus kinase 2, and tyrosine phosphorylation of the intracellular domain of PRLr. Knockdown of PKM2 attenuated PRL-stimulated cell proliferation. The extent of this proliferation was rescued by the knock-in of the wild-type PKM2 but not of its mutant insensitive to PRL-mediated inhibition. We discuss a hypothesis that the inhibition of PKM2 by PRL contributes to the PRL-stimulated cell proliferation.

Publication types

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

MeSH terms

  • Animals
  • Breast Neoplasms / metabolism
  • Cell Growth Processes / drug effects
  • Cell Growth Processes / physiology
  • Cell Line
  • Cell Line, Tumor
  • Gene Knock-In Techniques
  • Gene Knockdown Techniques
  • Humans
  • Janus Kinase 2 / metabolism
  • Lactic Acid / metabolism
  • Phosphorylation
  • Prolactin / pharmacology*
  • Pyruvate Kinase / antagonists & inhibitors*
  • Pyruvate Kinase / genetics
  • Pyruvate Kinase / metabolism
  • Rats
  • Receptors, Prolactin / genetics
  • Receptors, Prolactin / metabolism
  • Signal Transduction / drug effects
  • Tyrosine / metabolism

Substances

  • Receptors, Prolactin
  • Lactic Acid
  • Tyrosine
  • Prolactin
  • Pyruvate Kinase
  • JAK2 protein, human
  • Janus Kinase 2