Macrophage proliferation is regulated through CSF-1 receptor tyrosines 544, 559, and 807

J Biol Chem. 2012 Apr 20;287(17):13694-704. doi: 10.1074/jbc.M112.355610. Epub 2012 Feb 28.

Abstract

Colony-stimulating factor-1 (CSF-1)-stimulated CSF-1 receptor (CSF-1R) tyrosine phosphorylation initiates survival, proliferation, and differentiation signaling pathways in macrophages. Either activation loop Y807F or juxtamembrane domain (JMD) Y559F mutations severely compromise CSF-1-regulated proliferation and differentiation. YEF, a CSF-1R in which all eight tyrosines phosphorylated in the activated receptor were mutated to phenylalanine, lacks in vitro kinase activity and in vivo CSF-1-regulated tyrosine phosphorylation. The addition of Tyr-807 alone to the YEF backbone (Y807AB) led to CSF-1-independent but receptor kinase-dependent proliferation, without detectable activation loop Tyr-807 phosphorylation. The addition of Tyr-559 alone (Y559AB) supported a low level of CSF-1-independent proliferation that was slightly enhanced by CSF-1, indicating that Tyr-559 has a positive Tyr-807-independent effect. Consistent with the postulated autoinhibitory role of the JMD Tyr-559 and its relief by ligand-induced Tyr-559 phosphorylation, the addition of Tyr-559 to the Y807AB background suppressed proliferation in the absence of CSF-1, but restored most of the CSF-1-stimulated proliferation. Full restoration of kinase activation and proliferation required the additional add back of JMD Tyr-544. Inhibitor experiments indicate that the constitutive proliferation of Y807AB macrophages is mediated by the phosphatidylinositol 3-kinase (PI3K) and ERK1/2 pathways, whereas proliferation of WT and Y559,807AB macrophages is, in addition, contributed to by Src family kinase (SFK)-dependent pathways. Thus Tyr-807 confers sufficient kinase activity for strong CSF-1-independent proliferation, whereas Tyr-559 maintains the receptor in an inactive state. Tyr-559 phosphorylation releases this restraint and may also contribute to the CSF-1-regulated proliferative response by activating Src family kinase.

Publication types

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

MeSH terms

  • Animals
  • Cell Proliferation
  • Cell Survival
  • Cross-Linking Reagents / pharmacology
  • Gene Expression Regulation*
  • Humans
  • Macrophages / cytology*
  • Mice
  • Mutagenesis, Site-Directed
  • Mutation
  • Protein Structure, Tertiary
  • Receptor, Macrophage Colony-Stimulating Factor / chemistry*
  • Receptor, Macrophage Colony-Stimulating Factor / physiology*
  • Signal Transduction
  • Structure-Activity Relationship
  • Tyrosine / chemistry*

Substances

  • Cross-Linking Reagents
  • Tyrosine
  • Receptor, Macrophage Colony-Stimulating Factor