Long-term breast cancer response to CDK4/6 inhibition defined by TP53-mediated geroconversion

Cancer Cell. 2024 Nov 11;42(11):1919-1935.e9. doi: 10.1016/j.ccell.2024.09.009. Epub 2024 Oct 10.

Abstract

Inhibition of CDK4/6 kinases has led to improved outcomes in breast cancer. Nevertheless, only a minority of patients experience long-term disease control. Using a large, clinically annotated cohort of patients with metastatic hormone receptor-positive (HR+) breast cancer, we identify TP53 loss (27.6%) and MDM2 amplification (6.4%) to be associated with lack of long-term disease control. Human breast cancer models reveal that p53 loss does not alter CDK4/6 activity or G1 blockade but instead promotes drug-insensitive p130 phosphorylation by CDK2. The persistence of phospho-p130 prevents DREAM complex assembly, enabling cell-cycle re-entry and tumor progression. Inhibitors of CDK2 can overcome p53 loss, leading to geroconversion and manifestation of senescence phenotypes. Complete inhibition of both CDK4/6 and CDK2 kinases appears to be necessary to facilitate long-term response across genomically diverse HR+ breast cancers.

Keywords: CDK2; CDK4/6; breast cancer; cell cycle; cyclin dependent kinase; drug resistance; p53; quiescence; senescence.

MeSH terms

  • Animals
  • Breast Neoplasms* / drug therapy
  • Breast Neoplasms* / genetics
  • Breast Neoplasms* / metabolism
  • Breast Neoplasms* / pathology
  • Cell Line, Tumor
  • Cellular Senescence / drug effects
  • Cyclin-Dependent Kinase 2* / metabolism
  • Cyclin-Dependent Kinase 4* / antagonists & inhibitors
  • Cyclin-Dependent Kinase 4* / metabolism
  • Cyclin-Dependent Kinase 6* / antagonists & inhibitors
  • Cyclin-Dependent Kinase 6* / metabolism
  • Female
  • Humans
  • Mice
  • Phosphorylation
  • Protein Kinase Inhibitors / pharmacology
  • Protein Kinase Inhibitors / therapeutic use
  • Proto-Oncogene Proteins c-mdm2 / antagonists & inhibitors
  • Proto-Oncogene Proteins c-mdm2 / genetics
  • Proto-Oncogene Proteins c-mdm2 / metabolism
  • Tumor Suppressor Protein p53* / genetics
  • Tumor Suppressor Protein p53* / metabolism

Substances

  • Cyclin-Dependent Kinase 6
  • Cyclin-Dependent Kinase 4
  • Tumor Suppressor Protein p53
  • CDK6 protein, human
  • CDK4 protein, human
  • Cyclin-Dependent Kinase 2
  • TP53 protein, human
  • CDK2 protein, human
  • Protein Kinase Inhibitors
  • Proto-Oncogene Proteins c-mdm2
  • MDM2 protein, human