Purpose: We aimed to evaluate the feasibility of using streptavidin-biotin- based pretargeting for positron emission tomography (PET) imaging of hypoxia-inducible factor (HIF)-1-active tumors. Procedures: We used POS, a genetically engineered form of streptavidin that selectively stabilizes in HIF-1-active cells, and (4- 18F-fluorobenzoyl)norbiotinamide ( 18F-FBB), a radiolabeled biotin derivative, for performing a biodistribution study and for PET imaging. The tumoral 18F-FBB accumulation was compared to the HIF-1-dependent luciferase bioluminescence and HIF-1a immunohistochemical signal. Results: 18F-FBB accumulation was observed in POS-pretargeted tumors in mice (2.85±0.55% injected dose per gram at 3 h), and clear PET images were obtained at the same time point. The tumoral 18F-FBB accumulation positively correlated with luciferase bioluminescence (R=0.72, P<0.05), and most of the area showing 18F-FBB accumulation corresponded to HIF-1a-positive areas. Conclusion: Pretargeting with POS and 18F-FBB is an effective approach for PET imaging of HIF-1-active areas in tumors.
- F-labeled biotin derivative
- Hypoxia-inducible factor-1 (HIF-1)
- Oxygen-dependent degradation domain (ODD)
- Tumor hypoxia
ASJC Scopus subject areas
- Radiology Nuclear Medicine and imaging
- Cancer Research