Reporter PET Images Bortezomib Treatment-Mediated Suppression of Cancer Cell Proteasome Activity

Sci Rep. 2018 Aug 16;8(1):12290. doi: 10.1038/s41598-018-29642-w.

Abstract

Proteasomal protein degradation is a promising target for cancer therapy. Here, we developed a positron emission tomography (PET) technique based on the sodium-iodide symporter (NIS) gene fused with the carboxyl-terminal of ornithine decarboxylase (cODC) that noninvasively images cancer cells with inhibited proteasome activity. A retroviral vector was constructed in which the murine cODC degron was fused to the human NIS gene (NIS-cODC). Transiently transduced CT26 and HT29 colon cancer cells and stably expressing CT26/NIS-cODC cells were prepared. In cancer cells transiently transduced with NIS-cODC, NIS expression and transport activity was low at baseline, but NIS protein and 125I uptake was significantly increased by inhibition of proteasome activity with bortezomib. Stable CT26/NIS-cODC cells also showed increased cytosolic and membrane NIS by bortezomib, and four different stable clones displayed bortezomib dose-dependent stimulation of 125I and 99mTc-04- uptake. Importantly, bortezomib dose-dependently suppressed survival of CT26/NIS-cODC clones in a manner that closely correlated to the magnitudes of 125I and 99mTc-04- uptake. CT26/NIS-cODC tumors of bortezomib-treated mice demonstrated greater 124I uptake on PET images and increased NIS expression on tissue staining compared to vehicle-injected animals. NIS-cODC PET imaging may allow noninvasive quantitative monitoring of proteasome activity in cancer cells treated with bortezomib.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Bortezomib / pharmacology*
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Colonic Neoplasms / diagnostic imaging
  • Colonic Neoplasms / enzymology*
  • Colonic Neoplasms / pathology
  • Genes, Reporter*
  • Humans
  • Iodine Radioisotopes / administration & dosage
  • Mice
  • Positron-Emission Tomography*
  • Proteasome Endopeptidase Complex / metabolism*
  • Proteasome Inhibitors / pharmacology*
  • Symporters / genetics
  • Xenograft Model Antitumor Assays

Substances

  • Antineoplastic Agents
  • Iodine Radioisotopes
  • Iodine-124
  • Proteasome Inhibitors
  • Symporters
  • sodium-iodide symporter
  • Bortezomib
  • Proteasome Endopeptidase Complex