Non-invasive PET imaging of EGFR degradation induced by a heat shock protein 90 inhibitor

Mol Imaging Biol. 2008 Mar-Apr;10(2):99-106. doi: 10.1007/s11307-007-0123-2. Epub 2007 Dec 22.

Abstract

Purpose: The aim of this study is to non-invasively monitor the epidermal growth factor receptor (EGFR) response to a Hsp90 inhibitor-17-AAG treatment in a PC-3 prostate cancer model.

Procedures: Nude mice bearing PC-3 tumor were injected intraperitoneally with 17-AAG and then imaged with micro positron emission tomography (microPET) using (64)Cu-DOTA-cetuximab. Biodistribution studies, immunofluorescence staining, and Western blot were performed to validate the microPET results.

Results: PC-3 cells are sensitive to 17-AAG treatment in a dose-dependent manner. Quantitative microPET showed that (64)Cu-DOTA-cetuximab has prominent tumor activity accumulation in untreated tumors (14.6 +/- 2.6%ID/g) but significantly lower uptake in 17-AAG-treated tumors (8.9 +/- 1.6% ID/g) at 24 h post-injection. Both immunofluorescence staining and Western blot confirmed the significantly lower EGFR expression level in the tumor tissue upon 17-AAG treatment.

Conclusions: The early response to anti-Hsp90 therapy was successfully monitored by quantitative PET using (64)Cu-DOTA-cetuximab, which indicates that this approach may be valuable in monitoring the therapeutic response to Hsp90 inhibitor 17-AAG in EGFR-positive cancer patients.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Animals
  • Antibodies, Monoclonal / pharmacokinetics
  • Antibodies, Monoclonal / pharmacology
  • Antibodies, Monoclonal, Humanized
  • Antineoplastic Agents / pharmacokinetics
  • Antineoplastic Agents / pharmacology
  • Benzoquinones / pharmacokinetics
  • Benzoquinones / pharmacology*
  • Cell Death / drug effects
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cetuximab
  • ErbB Receptors / metabolism*
  • Fluorescent Antibody Technique
  • HSP90 Heat-Shock Proteins / antagonists & inhibitors*
  • Heterocyclic Compounds, 1-Ring / pharmacokinetics
  • Heterocyclic Compounds, 1-Ring / pharmacology
  • Humans
  • Lactams, Macrocyclic / pharmacokinetics
  • Lactams, Macrocyclic / pharmacology*
  • Mice
  • Mice, Nude
  • Neoplasm Transplantation
  • Positron-Emission Tomography / methods*
  • Protein Processing, Post-Translational / drug effects*
  • Tissue Distribution / drug effects

Substances

  • Antibodies, Monoclonal
  • Antibodies, Monoclonal, Humanized
  • Antineoplastic Agents
  • Benzoquinones
  • HSP90 Heat-Shock Proteins
  • Heterocyclic Compounds, 1-Ring
  • Lactams, Macrocyclic
  • 1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid
  • tanespimycin
  • ErbB Receptors
  • Cetuximab