First PCNA-directed PET tracer built from AOH1996 images glioma in mice

RadiopharmaceuticalsOncologyNeuroscience
  • Fluorine-18 tracer [18F]FPON, derived from the clinical PCNA inhibitor AOH1996, enables noninvasive imaging of a target tied to glioma stem cells and therapy resistance.
  • It binds PCNA like the parent drug and is made in one radiolabeling step, in modest yield and high purity.
  • The tracer enters the brain and stays largely intact; in orthotopic glioma xenografts uptake was specific, blocked by AOH1996, supporting companion-diagnostic use.
💡 Points Based on the abstract

Blocking by AOH1996 shows target-mediated uptake, but PCNA is abundant in every cycling cell, so the decisive number is tumor-to-normal-brain contrast, not absolute uptake. Controls to ask for: an inactive analog as a negative control, logD and P-gp efflux data for the fluorinated analog, and a non-proliferative lesion to test whether the signal tracks proliferation or just disrupted BBB.

Design, Synthesis, and Preclinical Evaluation of [ 18 F]FPON, a First-In-Class PET Tracer Targeting Proliferating Cell Nuclear Antigen for Glioblastoma Imaging ↗