Design and synthesis of antiangiogenic/heparin-binding arginine dendrimer mimicking the surface of endostatin

被引：55

作者：

Kasai, S

Nagasawa, H

Shimamura, M

Uto, Y

Hori, H

机构：

[1] Univ Tokushima, Fac Engn, Dept Biol Sci & Technol, Tokushima 7708506, Japan

[2] Tokyo Metropolitan Inst Med Sci, Dept Mol Oncol, Bunkyo Ku, Tokyo 1138613, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 06期

关键词：

D O I：

10.1016/S0960-894X(02)00066-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 TX1943 with eight arginine residues, and has stronger in vivo antiangiogenic activity at 10 mug/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. (C) 2002 Elsevier Science Ltd. All rights reserved.

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页码：951 / 954

页数：4

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