Background: Itraconazole is a widely used antifungal drug that was recently found to possess potent antiangiogenic activity. Results: We report here that itraconazole caused accumulation of immature N-glycans on VEGFR2 and inhibited VEGFR2 trafficking and signaling. Conclusion: These results suggest that itraconazole interferes with VEGFR2 trafficking, glycosylation, and signaling activity. Significance: Itraconazole possesses unique antiangiogenic potential through targeting multiple pathways that are essential for angiogenesis.
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Nacev et al. (2011) studied this question.
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