Novel insights into the molecular mechanisms governing Mdm2 ubiquitination and destruction

Oncotarget. 2010 Nov;1(7):685-90. doi: 10.18632/oncotarget.101011.

Abstract

The Mdm2/p53 pathway is compromised in more than 50% of all human cancers, therefore it is an intensive area of research to understand the upstream regulatory pathways governing Mdm2/p53 activity. Mdm2 is frequently overexpressed in human cancers while the molecular mechanisms underlying the timely destruction of Mdm2 remain unclear. We recently reported that Casein Kinase I phosphorylates Mdm2 at multiple sites to trigger Mdm2 interaction with, and subsequent ubiquitination and destruction by the SCF(β-TRCP) E3 ubiquitin ligase. We also demonstrated that the E3 ligase activity-deficient Mdm2 was still unstable in the G1 phase and could be efficiently degraded by SCF(β-TRCP). Thus our finding expands the current knowledge on how Mdm2 is tightly regulated by both self- and SCF(β-TRCP)-dependent ubiquitination to control p53 activity in response to stress. It further indicates that loss of β-TRCP or Casein Kinase I function contributes to elevated Mdm2 expression that is frequently found in various types of tumors.

Publication types

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

MeSH terms

  • Animals
  • Casein Kinase I / genetics
  • Casein Kinase I / metabolism
  • Humans
  • Models, Biological
  • Neoplasms / genetics
  • Neoplasms / metabolism
  • Phosphorylation / genetics
  • Protein Processing, Post-Translational / genetics*
  • Proto-Oncogene Proteins c-mdm2 / metabolism*
  • SKP Cullin F-Box Protein Ligases / genetics
  • SKP Cullin F-Box Protein Ligases / metabolism
  • Signal Transduction / genetics
  • Signal Transduction / physiology
  • Tumor Suppressor Protein p53 / metabolism
  • Tumor Suppressor Protein p53 / physiology
  • Ubiquitination / genetics*

Substances

  • Tumor Suppressor Protein p53
  • MDM2 protein, human
  • Proto-Oncogene Proteins c-mdm2
  • SKP Cullin F-Box Protein Ligases
  • Casein Kinase I