Design and synthesis of antiangiogenic/heparin-binding arginine dendrimer mimicking the surface of endostatin.
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.
Kasai
Soko
S
Department of Biological Science and Technology, Faculty of Engineering, The University of Tokushima, Minamijosanjimacho-2, 770-8506, Tokushima, Japan
Nagasawa
Hideko
H
Shimamura
Mariko
M
Uto
Yoshihiro
Y
Hori
Hitoshi
H
D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D001120:Arginine / Q000737:chemistry / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects; D002460:Cell Line; D002642:Chick Embryo; D003094:Collagen / Q000737:chemistry*; D015195:Drug Design; D043169:Endostatins; D006493:Heparin / Q000378:metabolism*; D018716:Molecular Mimicry; D018919:Neovascularization, Physiologic / Q000187:drug effects; D010446:Peptide Fragments / Q000737:chemistry*; D051381:Rats; D013329:Structure-Activity Relationship
D020533:Angiogenesis Inhibitors; D043169:Endostatins; D010446:Peptide Fragments; D006493:Heparin; D003094:Collagen; D001120:Arginine