Cannabinoid receptor 1 is a potential drug target for treatment of translocation-positive rhabdomyosarcoma

Mol Cancer Ther. 2009 Jul;8(7):1838-45. doi: 10.1158/1535-7163.MCT-08-1147. Epub 2009 Jun 9.

Abstract

Gene expression profiling has revealed that the gene coding for cannabinoid receptor 1 (CB1) is highly up-regulated in rhabdomyosarcoma biopsies bearing the typical chromosomal translocations PAX3/FKHR or PAX7/FKHR. Because cannabinoid receptor agonists are capable of reducing proliferation and inducing apoptosis in diverse cancer cells such as glioma, breast cancer, and melanoma, we evaluated whether CB1 is a potential drug target in rhabdomyosarcoma. Our study shows that treatment with the cannabinoid receptor agonists HU210 and Delta(9)-tetrahydrocannabinol lowers the viability of translocation-positive rhabdomyosarcoma cells through the induction of apoptosis. This effect relies on inhibition of AKT signaling and induction of the stress-associated transcription factor p8 because small interfering RNA-mediated down-regulation of p8 rescued cell viability upon cannabinoid treatment. Finally, treatment of xenografts with HU210 led to a significant suppression of tumor growth in vivo. These results support the notion that cannabinoid receptor agonists could represent a novel targeted approach for treatment of translocation-positive rhabdomyosarcoma.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apoptosis / drug effects*
  • Basic Helix-Loop-Helix Transcription Factors / genetics
  • Basic Helix-Loop-Helix Transcription Factors / metabolism
  • Blotting, Western
  • Cell Proliferation / drug effects
  • Dronabinol / analogs & derivatives*
  • Dronabinol / pharmacology*
  • Female
  • Glycogen Synthase Kinase 3 / genetics
  • Glycogen Synthase Kinase 3 / metabolism
  • Glycogen Synthase Kinase 3 beta
  • Humans
  • Immunoenzyme Techniques
  • Mice
  • Mice, Inbred NOD
  • Mice, SCID
  • Neoplasm Proteins / genetics
  • Neoplasm Proteins / metabolism
  • Oncogene Proteins, Fusion / genetics
  • PAX7 Transcription Factor / genetics
  • Proto-Oncogene Proteins c-akt / genetics
  • Proto-Oncogene Proteins c-akt / metabolism
  • RNA, Messenger / genetics
  • RNA, Messenger / metabolism
  • Receptor, Cannabinoid, CB1 / antagonists & inhibitors*
  • Receptor, Cannabinoid, CB1 / genetics
  • Receptor, Cannabinoid, CB1 / metabolism
  • Receptors, Interleukin-2 / physiology
  • Reverse Transcriptase Polymerase Chain Reaction
  • Rhabdomyosarcoma / genetics
  • Rhabdomyosarcoma / metabolism
  • Rhabdomyosarcoma / pathology*
  • Translocation, Genetic*
  • Tumor Cells, Cultured
  • Xenograft Model Antitumor Assays

Substances

  • Basic Helix-Loop-Helix Transcription Factors
  • NUPR1 protein, human
  • Neoplasm Proteins
  • Oncogene Proteins, Fusion
  • PAX3-FKHR fusion protein, human
  • PAX7 Transcription Factor
  • PAX7 protein, human
  • RNA, Messenger
  • Receptor, Cannabinoid, CB1
  • Receptors, Interleukin-2
  • Dronabinol
  • Glycogen Synthase Kinase 3 beta
  • Proto-Oncogene Proteins c-akt
  • Glycogen Synthase Kinase 3
  • HU 211