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| Content Provider | Springer Nature Link |
|---|---|
| Author | Byun, Youngro Park, Kyeongsoon Kim, Sung Eun Chin, Jungwook Lee, Hanna |
| Copyright Year | 2012 |
| Abstract | Therapeutic target for over-expressed α$_{v}$β$_{3}$ integrins in angiogenic endothelial cells and tumors is one of the promising approaches for cancer imaging and therapy. In the previous study, we demonstrated that heparin–lithocholic acid functionalized with cyclic RGDyK (cRGD–HL) had potent angiogenesis inhibition and tumor regression effects. The aim of this study is to validate the targeting property and specificity of cRGD–HL to α$_{v}$β$_{3}$ integrin-expressing endothelial cells and tumor tissues by Cy5.5-labeled cRGDyK (RGD-Cy5.5) as α$_{v}$β$_{3}$ integrin imaging agent and near-infrared fluorescence (NIRF) imaging systems. In this study, we demonstrated that cRGD–HL markedly inhibited the binding of fluorescein-labeled α$_{v}$β$_{3}$ antibody to α$_{v}$β$_{3}$ integrin-expressing endothelial cells when compared to non-functionalized heparin derivatives. Furthermore, in vivo NIRF images showed that cRGD–HL could decrease the NIRF signal intensities in both α$_{v}$β$_{3}$ integrin-positive tumor (U87 MG) and α$_{v}$β$_{3}$ integrin-negative tumor (SCC7) more effectively than non-functionalized heparin derivatives could. Therefore, with the help of α$_{v}$β$_{3}$ integrin imaging agent and NIRF imaging systems, we verified that the functionalized cRGD–HL has much stronger tumor targeting property and specificity against α$_{v}$β$_{3}$ integrin-expressing endothelial cells and tumors than non-functionalized heparin derivatives. Also, we believe that cRGD–HL will be useful and give affirmative outcomes for the treatment of angiogenesis-related diseases. |
| Starting Page | 9 |
| Ending Page | 14 |
| Page Count | 6 |
| File Format | |
| ISSN | 20935552 |
| Journal | Journal of Pharmaceutical Investigation |
| Volume Number | 42 |
| Issue Number | 1 |
| e-ISSN | 20936214 |
| Language | English |
| Publisher | Springer Netherlands |
| Publisher Date | 2012-02-02 |
| Publisher Place | Dordrecht |
| Access Restriction | One Nation One Subscription (ONOS) |
| Subject Keyword | α$_{v}$β$_{3}$ Integrin Heparin derivative Tumor targeting Optical imaging Cyclic RGD Biomedicine general |
| Content Type | Text |
| Resource Type | Article |
| Subject | Pharmaceutical Science |
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