Synergistic and additive effect of retinoic acid in circumventing resistance to p53 restoration

Proc Natl Acad Sci U S A. 2018 Feb 27;115(9):2198-2203. doi: 10.1073/pnas.1719001115. Epub 2018 Feb 13.

Abstract

TP53 mutations occur in ∼50% of all human tumors, with increased frequency in aggressive cancers that are notoriously difficult to treat. Additionally, p53 missense mutations are remarkably predictive of refractoriness to chemo/radiotherapy in various malignancies. These observations have led to the development of mutant p53-targeting agents that restore p53 function. An important unknown is which p53-mutant tumors will respond to p53 reactivation-based therapies. Here, we found a heterogeneous impact on therapeutic response to p53 restoration, suggesting that it will unlikely be effective as a monotherapy. Through gene expression profiling of p53R172H -mutant lymphomas, we identified retinoic acid receptor gamma (RARγ) as an actionable target and demonstrated that pharmacological activation of RARγ with a synthetic retinoid sensitizes resistant p53-mutant lymphomas to p53 restoration, while additively improving outcome and survival in inherently sensitive tumors.

Keywords: TNF; mutant p53; p53 restoration; retinoic acid; therapeutic response.

Publication types

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

MeSH terms

  • Animals
  • Antineoplastic Agents, Hormonal / administration & dosage
  • Antineoplastic Agents, Hormonal / pharmacokinetics
  • Antineoplastic Agents, Hormonal / pharmacology
  • Drug Resistance, Neoplasm
  • Drug Synergism
  • Gene Expression Regulation, Neoplastic / drug effects*
  • Mice
  • Mice, Inbred Strains
  • Mutation, Missense
  • Neoplasms, Experimental / drug therapy*
  • Retinoids / administration & dosage
  • Retinoids / pharmacokinetics
  • Retinoids / pharmacology*
  • Tamoxifen / administration & dosage
  • Tamoxifen / pharmacokinetics
  • Tamoxifen / pharmacology*
  • Transcriptome
  • Tumor Necrosis Factor-alpha / metabolism
  • Tumor Suppressor Protein p53 / genetics
  • Tumor Suppressor Protein p53 / metabolism*

Substances

  • Antineoplastic Agents, Hormonal
  • CD 437
  • Retinoids
  • Tumor Necrosis Factor-alpha
  • Tumor Suppressor Protein p53
  • Tamoxifen