Azide-bearing VEGFR2 inhibitors switch on under green light in the retina
- Azido-functionalized VEGFR2 inhibitors EYE1090 and EYE1118 bind the receptor in a light-triggered way while staying potent in the dark.
- Green light that reaches the human retina, including in older eyes, boosted their anti-angiogenic activity in vitro.
- Given orally, both suppressed VEGF-induced retinal leakage in rats and shrank lesions in a mouse choroidal neovascularization model without acute liver toxicity.
💡 Points
An azide as the photo-switch is a neat, small-footprint handle on a classic kinase scaffold. The appeal is spatial selectivity: systemic exposure with activity concentrated where light focuses. I'd probe how much dark activity remains, which matters for off-target VEGFR2 effects elsewhere, and the photoproduct's fate.
Three Nitrogen Atoms Turn Old Kinase Inhibitors Into New Targetable Remedy ↗