Site-specific proteasome phosphorylation controls cell proliferation and tumorigenesis

Nat Cell Biol. 2016 Feb;18(2):202-12. doi: 10.1038/ncb3289. Epub 2015 Dec 14.

Abstract

Despite the fundamental importance of proteasomal degradation in cells, little is known about whether and how the 26S proteasome itself is regulated in coordination with various physiological processes. Here we show that the proteasome is dynamically phosphorylated during the cell cycle at Thr 25 of the 19S subunit Rpt3. CRISPR/Cas9-mediated genome editing, RNA interference and biochemical studies demonstrate that blocking Rpt3-Thr25 phosphorylation markedly impairs proteasome activity and impedes cell proliferation. Through a kinome-wide screen, we have identified dual-specificity tyrosine-regulated kinase 2 (DYRK2) as the primary kinase that phosphorylates Rpt3-Thr25, leading to enhanced substrate translocation and degradation. Importantly, loss of the single phosphorylation of Rpt3-Thr25 or knockout of DYRK2 significantly inhibits tumour formation by proteasome-addicted human breast cancer cells in mice. These findings define an important mechanism for proteasome regulation and demonstrate the biological significance of proteasome phosphorylation in regulating cell proliferation and tumorigenesis.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • ATPases Associated with Diverse Cellular Activities
  • Animals
  • Breast Neoplasms / enzymology*
  • Breast Neoplasms / genetics
  • Breast Neoplasms / pathology
  • CRISPR-Cas Systems
  • Cell Cycle
  • Cell Line, Tumor
  • Cell Proliferation*
  • Cell Transformation, Neoplastic / genetics
  • Cell Transformation, Neoplastic / metabolism*
  • Cell Transformation, Neoplastic / pathology
  • Dyrk Kinases
  • Female
  • Gene Expression Regulation, Neoplastic
  • Heterografts
  • Humans
  • Mice, Nude
  • Phosphorylation
  • Proteasome Endopeptidase Complex / genetics
  • Proteasome Endopeptidase Complex / metabolism*
  • Protein Serine-Threonine Kinases / genetics
  • Protein Serine-Threonine Kinases / metabolism*
  • Protein-Tyrosine Kinases / genetics
  • Protein-Tyrosine Kinases / metabolism*
  • Proteolysis
  • RNA Interference
  • Signal Transduction
  • Threonine
  • Time Factors
  • Transfection
  • Tumor Burden

Substances

  • Threonine
  • Protein-Tyrosine Kinases
  • Protein Serine-Threonine Kinases
  • PSMC4 protein, human
  • Proteasome Endopeptidase Complex
  • ATPases Associated with Diverse Cellular Activities