US9403869: Alpha5beta1 integrin binding rgd-lipopeptides with gene transfer activities

The invention provides synthesis of a novel series of cationic lipopeptides with integrin-binding RGD functionalities. The invention also provides high L27 (transformed S180, mouse sarcoma cells) cell tropic gene transfer properties of these novel RGD-lipopeptides. Since L27 cell surface contains over expressed integrins, the present class of lipopeptides with integrin-binding RGD ligands are likely to find future applications in targeting anti-cancer genes/drugs to the endothelial cells of tumor vasculatures (possessing over expressed integrins).