4.7 Article

Novel Peptide-Specific Quantitative Structure-Activity Relationship (QSAR) Analysis Applied to Collagen IV Peptides with Antiangiogenic Activity

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JOURNAL OF MEDICINAL CHEMISTRY
卷 54, 期 19, 页码 6492-6500

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AMER CHEMICAL SOC
DOI: 10.1021/jm200114f

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  1. NIH [R01 CA138264, R01 HL101200, U54RR020839]

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Angiogenesis is the growth of new blood vessels from existing vasculature. Excessive vascularization is associated with a number of diseases including cancer. Antiangiogenic therapies have the potential to stunt cancer progression. Peptides derived from type IV collagen are potent inhibitors of angiogenesis. We wanted to gain a better understanding of collagen IV structure-activity relationships using a ligand-based approach. We developed novel peptide-specific QSAR models to study the activity of the peptides in endothelial cell proliferation, migration, and adhesion inhibition assays. We found that the models produced quantitatively accurate predictions of activity and provided insight into collagen IV derived peptide structure-activity relationships.

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