Collective inhibition of pRB family proteins by phosphorylation in cells with p16INK4a loss or cyclin E overexpression

J Biol Chem. 2001 Apr 6;276(14):11362-70. doi: 10.1074/jbc.M007992200. Epub 2001 Jan 4.

Abstract

The activity of the retinoblastoma protein pRB is regulated by phosphorylation that is mediated by G(1) cyclin-associated cyclin-dependent kinases (CDKs). Since the pRB-related pocket proteins p107 and p130 share general structures and biological functions with pRB, their activity is also considered to be regulated by phosphorylation. In this work, we generated phosphorylation-resistant p107 and p130 molecules by replacing potential cyclin-CDK phosphorylation sites with non-phosphorylatable alanine residues. These phosphorylation-resistant mutants retained the ability to bind E2F and cyclin. Upon introduction into p16(INK4a)-deficient U2-OS osteosarcoma cells, in which cyclin D-CDK4/6 is dysregulated, the phosphorylation-resistant mutants, but not wild-type p107 or p130, were capable of inhibiting cell proliferation. Furthermore, when ectopically expressed in pRB-deficient SAOS-2 osteosarcoma cells, the wild-type as well as the phosphorylation-resistant pRB family proteins were capable of inducing large flat cells. The flat cell-inducing activity of the wild-type proteins, but not that of the phosphorylation-resistant mutants, was abolished by coexpressing cyclin E. Our results indicate that the elevated cyclin D- or cyclin E-associated kinase leads to systemic inactivation of the pRB family proteins and suggest that dysregulation of the pRB kinase provokes an aberrant cell cycle in a broader range of cell types than those induced by genetic inactivation of the RB gene.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cyclin E / biosynthesis*
  • Cyclin E / genetics
  • Cyclin-Dependent Kinase Inhibitor p16 / genetics
  • Cyclin-Dependent Kinase Inhibitor p16 / metabolism*
  • Gene Deletion
  • Gene Expression Regulation, Neoplastic
  • Humans
  • Retinoblastoma Protein / metabolism*
  • Tumor Cells, Cultured

Substances

  • Cyclin E
  • Cyclin-Dependent Kinase Inhibitor p16
  • Retinoblastoma Protein