Cathepsin K inhibition-induced mitochondrial ROS enhances sensitivity of cancer cells to anti-cancer drugs through USP27x-mediated Bim protein stabilization

Redox Biol. 2020 Feb:30:101422. doi: 10.1016/j.redox.2019.101422. Epub 2019 Dec 31.

Abstract

Cathepsin K (Cat K) is expressed in cancer cells, but the effect of Cat K on apoptosis is still elusive. Here, we showed that inhibition of Cat K sensitized the human carcinoma cells to anti-cancer drug through up-regulation of Bim. Inhibition of Cat K increased USP27x expression, and knock down of USP27x markedly blocked Cat K-induced up-regulation of Bim expression. Furthermore, inhibition of Cat K induced proteasome-dependent degradation of regulatory associated protein of mammalian target of rapamycin (Raptor). Down-regulation of Raptor expression increased mitochondrial ROS production, and mitochondria specific superoxide scavengers prevented USP27x-mediated stabilization of Bim by inhibition of Cat K. Moreover, combined treatment with Cat K inhibitor (odanacatib) and tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) reduced tumor growth and induced cell death in a xenograft model. Our results demonstrate that Cat K inhibition enhances anti-cancer drug sensitivity through USP27x-mediated the up-regulation of Bim via the down-regulation of Raptor.

Keywords: Apoptosis; Bim; Cathepsin K; Mitochondria; Raptor; USP27x.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Bcl-2-Like Protein 11 / chemistry*
  • Bcl-2-Like Protein 11 / metabolism
  • Biphenyl Compounds / pharmacology*
  • Cathepsin K / antagonists & inhibitors
  • Cathepsin K / metabolism*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Drug Synergism
  • Gene Expression Regulation, Neoplastic / drug effects
  • HeLa Cells
  • Humans
  • Kidney Neoplasms / drug therapy*
  • Kidney Neoplasms / metabolism
  • Male
  • Mice
  • Mitochondria / metabolism*
  • Protein Stability
  • Reactive Oxygen Species / metabolism
  • TNF-Related Apoptosis-Inducing Ligand / pharmacology
  • Ubiquitin-Specific Proteases / metabolism*
  • Xenograft Model Antitumor Assays

Substances

  • Antineoplastic Agents
  • BCL2L11 protein, human
  • Bcl-2-Like Protein 11
  • Biphenyl Compounds
  • Reactive Oxygen Species
  • TNF-Related Apoptosis-Inducing Ligand
  • USP27X protein, human
  • Ubiquitin-Specific Proteases
  • CTSK protein, human
  • Cathepsin K
  • odanacatib