Cancerous inhibitor of PP2A is targeted by natural compound celastrol for degradation in non-small-cell lung cancer

Carcinogenesis. 2014 Apr;35(4):905-14. doi: 10.1093/carcin/bgt395. Epub 2013 Nov 30.

Abstract

Celastrol binds CIP2A and enhances CIP2A-CHIP interaction, leading to ubiquitination/degradation of CIP2A and inhibition of lung cancer cells in vitro and in vivo. Celastrol potentiates cisplatin's efficacy by suppressing the CIP2A-Akt pathway, and therefore CIP2A inhibitors may represent novel therapeutics for cancer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Autoantigens / drug effects*
  • Autoantigens / metabolism
  • Biomarkers, Tumor / metabolism*
  • Carcinoma, Non-Small-Cell Lung / enzymology
  • Carcinoma, Non-Small-Cell Lung / metabolism*
  • Carcinoma, Non-Small-Cell Lung / pathology
  • Cell Line, Tumor
  • Humans
  • Intracellular Signaling Peptides and Proteins
  • Lung Neoplasms / enzymology
  • Lung Neoplasms / metabolism*
  • Lung Neoplasms / pathology
  • Membrane Proteins / drug effects*
  • Membrane Proteins / metabolism
  • Mice
  • Pentacyclic Triterpenes
  • Proteolysis
  • Triterpenes / pharmacology*
  • Ubiquitination

Substances

  • Autoantigens
  • Biomarkers, Tumor
  • CIP2A protein, human
  • Intracellular Signaling Peptides and Proteins
  • Membrane Proteins
  • Pentacyclic Triterpenes
  • Triterpenes
  • celastrol