Selective CDK9 knockdown sensitizes TRAIL response by suppression of antiapoptotic factors and NF-kappaB pathway

Apoptosis. 2023 Aug;28(7-8):1060-1075. doi: 10.1007/s10495-023-01842-4. Epub 2023 Apr 15.

Abstract

The aberrantly up-regulated CDK9 can be targeted for cancer therapy. The CDK inhibitor dinaciclib (Dina) has been found to drastically sensitizes cancer response to TRAIL-expressing extracellular vesicle (EV-T). However, the low selectivity of Dina has limited its application for cancer. We propose that CDK9-targeted siRNA (siCDK9) may be a good alternative to Dina. The siCDK9 molecules were encapsulated into EV-Ts to prepare a complexed nanodrug (siEV-T). It was shown to efficiently suppress CDK9 expression and overcome TRAIL resistance to induce strikingly augmented apoptosis in lung cancer both in vitro and in vivo, with a mechanism related to suppression of both anti-apoptotic factors and nuclear factor-kappa B pathway. Therefore, siEV-T potentially constitutes a novel, highly effective and safe therapy for cancers.

Keywords: CDK9 silencing; Cancer therapy; DR5; NF-κB; TRAIL-resistance.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Apoptosis
  • Cell Line, Tumor
  • Cyclin-Dependent Kinase 9 / genetics
  • Humans
  • Lung Neoplasms* / drug therapy
  • Lung Neoplasms* / genetics
  • Lung Neoplasms* / metabolism
  • NF-kappa B* / genetics
  • NF-kappa B* / metabolism
  • RNA, Small Interfering / genetics
  • Receptors, TNF-Related Apoptosis-Inducing Ligand / genetics
  • TNF-Related Apoptosis-Inducing Ligand / genetics
  • TNF-Related Apoptosis-Inducing Ligand / pharmacology

Substances

  • NF-kappa B
  • RNA, Small Interfering
  • TNF-Related Apoptosis-Inducing Ligand
  • Receptors, TNF-Related Apoptosis-Inducing Ligand
  • CDK9 protein, human
  • Cyclin-Dependent Kinase 9