Senescence induction in renal carcinoma cells by Nutlin-3: a potential therapeutic strategy based on MDM2 antagonism

Cancer Lett. 2014 Oct 28;353(2):211-9. doi: 10.1016/j.canlet.2014.07.024. Epub 2014 Jul 24.

Abstract

Although the role of p53 as a tumour suppressor in renal cell carcinoma (RCC) is unclear, our recent analysis suggests that increased wild-type p53 protein expression is associated with poor outcome. A growing body of evidence also suggests that p53 expression and increased co-expression of MDM2 are linked with poor prognosis in RCC. We have therefore examined whether an MDM2 antagonist; Nutlin-3, might rescue/increase p53 expression and induce growth inhibition or apoptosis in RCC cells that retain wild-type p53. We show that inhibition of p53 suppression by MDM2 in RCC cells promotes growth arrest and p53-dependent senescence - phenotypes known to mediate p53 tumour suppression in vivo. We propose that future investigations of therapeutic strategies for RCC should incorporate MDM2 antagonism as part of strategies aimed at rescuing/augmenting p53 tumour suppressor function.

Keywords: MDM2; Nutlin-3; Renal cell carcinoma; Senescence; Targeted therapy; p53.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Carcinoma, Renal Cell
  • Cell Line, Tumor
  • Cell Proliferation
  • Cellular Senescence
  • Gene Expression Regulation, Neoplastic
  • Humans
  • Imidazoles / pharmacology*
  • Kidney Neoplasms
  • Piperazines / pharmacology*
  • Proto-Oncogene Proteins c-mdm2 / antagonists & inhibitors*
  • Proto-Oncogene Proteins c-mdm2 / genetics
  • Proto-Oncogene Proteins c-mdm2 / metabolism
  • RNA, Messenger / genetics
  • RNA, Messenger / metabolism
  • Tumor Suppressor Protein p53 / metabolism

Substances

  • Antineoplastic Agents
  • Imidazoles
  • Piperazines
  • RNA, Messenger
  • TP53 protein, human
  • Tumor Suppressor Protein p53
  • nutlin 3
  • MDM2 protein, human
  • Proto-Oncogene Proteins c-mdm2