Discovery of Nonretinoid Antagonists of Retinol-Binding Protein 4 for the Treatment of Atrophic Age-Related Macular Degeneration and Stargardt Disease
Time: 4:00 pm
day: Day 1
Details:
- Antagonists of retinol-binding protein 4 (RBP4) impede ocular uptake of serum all-trans retinol and have been shown to reduce cytotoxic bisretinoid formation in the retinal pigment epithelium (RPE), which is associated with the pathogenesis of both atrophic age-related macular degeneration (AMD) and Stargardt disease
- Computer-assisted drug design based around several RBP4 protein crystal structures was used to help design and computationally evaluate novel nonretinoid RBP4 antagonists
- Potent RBP4 antagonists were identified with favorable drug-like characteristics that reduced circulating plasma RBP4 levels, demonstrating in vivo target engagement and potential as oral treatments for atrophic AMD and Stargardt disease
Speakers:
