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Molecular imaging of α v β 3 integrin has exhibited real potential to guide the appropriate use of anti-angiogenic therapies. However, an incomplete understanding of the factors that influence binding of α v β 3 integrin-specific radiotracers currently limits their use for assessing response to therapy in cancer patients. This study identifies two fundamental factors that modulate uptake of these radiotracers. Procedures Experiments were performed in prostate cancer (PC3) and glioblastoma (U87MG) cells, which differentially express α v β 3 integrin. α v β 3 integrin-specific radiotracers were used to investigate the effect of manipulating α v β 3 integrin expression or activation in cellular binding assays. β 3 integrin and α v β 3 integrin expression were measured by western blotting and flow cytometry, respectively. The effect of select pharmacological inhibitors on α v β 3 integrin activation and expression was also determined.

Binding of αvβ3 Integrin-Specific Radiotracers Is Modulated by Both Integrin Expression Level and Activation Status