The oncolytic peptide LTX-315 triggers necrotic cell death

Cell Cycle. 2015;14(21):3506-12. doi: 10.1080/15384101.2015.1093710.

Abstract

The oncolytic peptide LTX-315 has been designed for killing human cancer cells and turned out to stimulate anti-cancer immune responses when locally injected into tumors established in immunocompetent mice. Here, we investigated the question whether LTX-315 induces apoptosis or necrosis. Transmission electron microscopy or morphometric analysis of chromatin-stained tumor cells revealed that LTX-315 failed to induce apoptotic nuclear condensation and rather induced a necrotic phenotype. Accordingly, LTX-315 failed to stimulate the activation of caspase-3, and inhibition of caspases by means of Z-VAD-fmk was unable to reduce cell killing by LTX-315. In addition, 2 prominent inhibitors of regulated necrosis (necroptosis), namely, necrostatin-1 and cycosporin A, failed to reduce LTX-315-induced cell death. In conclusion, it appears that LTX-315 triggers unregulated necrosis, which may contribute to its pro-inflammatory and pro-immune effects.

Keywords: anticancer immunity, apoptotsis, necrosis, LTX-315.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Chloromethyl Ketones / pharmacology
  • Antineoplastic Agents / pharmacology*
  • Apoptosis
  • Bone Neoplasms / drug therapy*
  • Bone Neoplasms / metabolism
  • Bone Neoplasms / ultrastructure
  • Caspase Inhibitors / pharmacology
  • Cell Line, Tumor
  • Cyclosporine / pharmacology
  • Dose-Response Relationship, Drug
  • Humans
  • Imidazoles / pharmacology
  • Indoles / pharmacology
  • Microscopy, Electron, Transmission
  • Necrosis
  • Oligopeptides / pharmacology*
  • Osteosarcoma / drug therapy*
  • Osteosarcoma / metabolism
  • Osteosarcoma / ultrastructure
  • Time Factors

Substances

  • Amino Acid Chloromethyl Ketones
  • Antineoplastic Agents
  • Caspase Inhibitors
  • Imidazoles
  • Indoles
  • LTX-315
  • Oligopeptides
  • benzyloxycarbonylvalyl-alanyl-aspartyl fluoromethyl ketone
  • necrostatin-1
  • Cyclosporine