Understanding the pharmacological properties of a metabolic PET tracer in prostate cancer Academic Article Article uri icon


MeSH Major

  • Cardiology
  • Clinical Competence
  • Consensus
  • Diagnostic Self Evaluation
  • Educational Measurement
  • Emergency Medicine
  • Internship and Residency


  • Generally, solid tumors (>400 mm(3)) are inherently acidic, with more aggressive growth producing greater acidity. If the acidity could be targeted as a biomarker, it would provide a means to gauge the pace of tumor growth and degree of invasiveness, as well as providing a basis for predicting responses to pH-dependent chemotherapies. We have developed a (64)Cu pH (low) insertion peptide (pHLIP) for targeting, imaging, and quantifying acidic tumors by PET, and our findings reveal utility in assessing prostate tumors. The new pHLIP version limits indiscriminate healthy tissue binding, and we demonstrate its targeting of extracellular acidification in three different prostate cancer models, each with different vascularization and acid-extruding protein carbonic anhydrase IX (CAIX) expression. We then describe the tumor distribution of this radiotracer ex vivo, in association with blood perfusion and known biomarkers of acidity, such as hypoxia, lactate dehydrogenase A, and CAIX. We find that the probe reveals metabolic variations between and within tumors, and discriminates between necrotic and living tumor areas.

publication date

  • May 20, 2014



  • Academic Article


Digital Object Identifier (DOI)

  • 10.1073/pn

PubMed ID

  • 24785505

Additional Document Info

start page

  • 7254

end page

  • 9


  • 111


  • 20