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Design and synthesis of antiangiogenic/heparin-binding arginine dendrimer mimicking the surface of endostatin
Authors:Kasai Soko  Nagasawa Hideko  Shimamura Mariko  Uto Yoshihiro  Hori Hitoshi
Institution:Department of Biological Science and Technology, Faculty of Engineering, The University of Tokushima, Minamijosanjimacho-2, 770-8506, Tokushima, Japan
Abstract:We designed and synthesized the antiangiogenic arginine-rich dendrimers, TX-1943 and TX-1944, which mimic the surface structure of endostatin. TX-1944 containing 16 arginine residues is more similar in surface structure to endostatin than TX-1943 with eight arginine residues, and has stronger in vivo antiangiogenic activity at 10 microg/CAM in the chicken embryo chorioallantoic membrane (CAM) assay. TX-1944 also has stronger activity to bind heparin and to inhibit the growth of rat lung endothelial (RLE) cells than TX-1943.
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