Lipopeptide with a RGDK Tetrapeptide Sequence Can Selectively Target Genes to Proangiogenic α5β1 Integrin Receptor and Mouse Tumor Vasculature
- 28 October 2008
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 51 (22) , 7298-7302
- https://doi.org/10.1021/jm800915y
Abstract
Integrins, the major class of αβ heterodimeric transmembrane glycoprotein receptors, play crucial roles in mediating tumor angiogenesis. Genetic ablation experiments combined with use of antibodies/peptide ligands for blocking either α5 or β1 integrins have convincingly demonstrated α5β1 integrin to be unquestionably proangiogenic among the 24 known integrin receptors. Herein, we report on a novel RGDK-lipopeptide 1 that targets selectively α5β1 integrin and is capable of targeting genes to mouse tumor vasculatures.Keywords
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