Kinesin light chain 4 as a new target for lung cancer chemoresistance via targeted inhibition of checkpoint kinases in the DNA repair network

Cell Death Dis. 2020 May 26;11(5):398. doi: 10.1038/s41419-020-2592-z.

Abstract

The poor therapeutic efficacy of non-small cell lung cancer (NSCLC) is partly attributed to the acquisition of chemoresistance. To investigate the mechanism underlying this resistance, we examined the potential link between kinesin light chain 4 (KLC4), which we have previously reported to be associated with radioresistance in NSCLC, and sensitivity to chemotherapy in human lung cancer cell lines. KLC4 protein levels in lung cancer cells correlated with the degree of chemoresistance to cisplatin treatment. Furthermore, KLC4 silencing enhanced the cytotoxic effect of cisplatin by promoting DNA double-strand breaks and apoptosis. These effects were mediated by interaction with the checkpoint kinase CHK2, as KLC4 knockdown increased CHK2 activation, which was further enhanced in combination with cisplatin treatment. In addition, KLC4 and CHEK2 expression levels showed negative correlation in lung tumor samples from patients, and KLC4 overexpression correlated negatively with survival. Our results indicate a novel link between the KLC4 and CHK2 pathways regulating DNA damage response in chemoresistance, and highlight KLC4 as a candidate for developing lung cancer-specific drugs and customized targeted molecular therapy.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Apoptosis / drug effects
  • Cell Line, Tumor
  • Checkpoint Kinase 1 / antagonists & inhibitors*
  • Checkpoint Kinase 1 / metabolism
  • Checkpoint Kinase 2 / antagonists & inhibitors*
  • Checkpoint Kinase 2 / metabolism
  • Cisplatin / pharmacology
  • Colorectal Neoplasms / pathology
  • DNA Damage
  • DNA Repair* / drug effects
  • DNA-Activated Protein Kinase / metabolism
  • Down-Regulation / drug effects
  • Down-Regulation / genetics
  • Drug Resistance, Neoplasm* / drug effects
  • Etoposide / pharmacology
  • Gene Expression Regulation, Neoplastic / drug effects
  • Gene Knockdown Techniques
  • Gene Silencing / drug effects
  • Humans
  • Kinesins / genetics
  • Kinesins / metabolism*
  • Lung Neoplasms / drug therapy*
  • Lung Neoplasms / enzymology
  • Lung Neoplasms / genetics
  • Lung Neoplasms / pathology
  • Microtubule-Associated Proteins / metabolism*
  • Molecular Targeted Therapy*
  • Signal Transduction / drug effects

Substances

  • KLC4 protein, human
  • Microtubule-Associated Proteins
  • Etoposide
  • Checkpoint Kinase 2
  • CHEK1 protein, human
  • CHEK2 protein, human
  • Checkpoint Kinase 1
  • DNA-Activated Protein Kinase
  • PRKDC protein, human
  • Kinesins
  • Cisplatin