The G1-S transition is promoted by Rb degradation via the E3 ligase UBR5

Sci Adv. 2024 Oct 25;10(43):eadq6858. doi: 10.1126/sciadv.adq6858. Epub 2024 Oct 23.

Abstract

Mammalian cells make the decision to divide at the G1-S transition in response to diverse signals impinging on the retinoblastoma protein Rb, a cell cycle inhibitor and tumor suppressor. Passage through the G1-S transition is initially driven by Rb inactivation via phosphorylation and by Rb's decreasing concentration in G1. While many studies have identified the mechanisms of Rb phosphorylation, the mechanism underlying Rb's decreasing concentration in G1 was unknown. Here, we found that Rb's concentration decrease in G1 requires the E3 ubiquitin ligase UBR5. UBR5 knockout cells have increased Rb concentration in early G1, exhibited a lower G1-S transition rate, and are more sensitive to inhibition of cyclin-dependent kinase 4/6 (Cdk4/6). This last observation suggests that UBR5 inhibition can strengthen the efficacy of Cdk4/6 inhibitor-based cancer therapies.

MeSH terms

  • Cell Line, Tumor
  • Cyclin-Dependent Kinase 4* / antagonists & inhibitors
  • Cyclin-Dependent Kinase 4* / metabolism
  • Cyclin-Dependent Kinase 6 / genetics
  • Cyclin-Dependent Kinase 6 / metabolism
  • G1 Phase
  • Humans
  • Phosphorylation
  • Proteolysis
  • Retinoblastoma Protein* / genetics
  • Retinoblastoma Protein* / metabolism
  • S Phase
  • Ubiquitin-Protein Ligases* / genetics
  • Ubiquitin-Protein Ligases* / metabolism

Substances

  • Ubiquitin-Protein Ligases
  • UBR5 protein, human
  • Retinoblastoma Protein
  • Cyclin-Dependent Kinase 4
  • Cyclin-Dependent Kinase 6
  • CDK4 protein, human