Cyclic RGDyk-conjugated LMWH-taurocholate derivative as a targeting angiogenesis inhibitor

Title
Cyclic RGDyk-conjugated LMWH-taurocholate derivative as a targeting angiogenesis inhibitor
Authors
Asarasin Adulnirath정성우박주호황승림김지영Victor C. Yang김상윤문현태변영로
Keywords
Heparin-taurocholate; LMWH; cRGD; αvβ3 integrin; Angiogenesis inhibitor
Issue Date
2012-11
Publisher
Journal of controlled release
Citation
VOL 164, NO 1, 8-16
Abstract
LMWH-taurocholate derivative (LHT7) has been reported as a novel angiogenesis inhibitor, due to its ability to bind to several kinds of growth factors, which play critical roles in tumor angiogenesis. In this study, we have highlighted the enhanced antiangiogenic activity of LHT7, by using cyclic RGDyk (cRGD), a targeting moiety that was chemically conjugated to LHT7 via amide bond. The SPR study revealed that cRGD-LHT7 bound to αvβ3 integrin as strongly as cRGD, and it bound to VEGF as strongly as LHT7. Importantly, in vitro anti-angiogenesis studies revealed that cRGD-LHT7 had a significant inhibition effect on HUVEC tubular formation. Finally, cRGD-LHT7 showed a greater inhibitory efficiency on the tumor growth in the U87MG xenograft model than the original LHT7, which was owed to its ability to target the tumor cells. All of these findings demonstrated that cRGD-LHT7 targetedαvβ3 integrin-positive cancer cells and endothelial cells, resulting in a greater anti-angiogenesis effect on the solid tumors.
URI
http://pubs.kist.re.kr/handle/201004/45698
ISSN
01683659
Appears in Collections:
KIST Publication > Article
Files in This Item:
There are no files associated with this item.
Export
RIS (EndNote)
XLS (Excel)
XML


qrcode

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

BROWSE