Cyclic RGDyk-conjugated LMWH-taurocholate derivative as a targeting angiogenesis inhibitor
- Cyclic RGDyk-conjugated LMWH-taurocholate derivative as a targeting angiogenesis inhibitor
- Asarasin Adulnirath; 정성우; 박주호; 황승림; 김지영; Victor C. Yang; 김상윤; 문현태; 변영로
- Heparin-taurocholate; LMWH; cRGD; αvβ3 integrin; Angiogenesis inhibitor
- Issue Date
- Journal of controlled release
- VOL 164, NO 1, 8-16
- 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.
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