Reviving the guardian of the genome: Small molecule activators of p53

Pharmacol Ther. 2017 Oct:178:92-108. doi: 10.1016/j.pharmthera.2017.03.013. Epub 2017 Mar 27.

Abstract

The tumor suppressor p53 is one of the most important proteins for protection of genomic stability and cancer prevention. Cancers often inactivate it by either mutating its gene or disabling its function. Thus, activating p53 becomes an attractive approach for the development of molecule-based anti-cancer therapy. The past decade and half have witnessed tremendous progress in this area. This essay offers readers with a grand review on this progress with updated information about small molecule activators of p53 either still at bench work or in clinical trials.

Keywords: Drug discovery; Inauhzin; MDM2; MDMX; Small molecules; p53.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / therapeutic use
  • Genome
  • Humans
  • Mutation
  • Neoplasms / drug therapy
  • Neoplasms / genetics*
  • Tumor Suppressor Protein p53 / genetics*

Substances

  • Antineoplastic Agents
  • Tumor Suppressor Protein p53