Brandwijk Ricardo J M G E, Mulder Willem J M, Nicolay Klaas, Mayo Kevin H, Thijssen Victor L J L, Griffioen Arjan W
Angiogenesis Laboratory, Research Institute Growth and Development (GROW), Department of Pathology, Maastricht University & University Hospital, Maastricht, The Netherlands.
Bioconjug Chem. 2007 May-Jun;18(3):785-90. doi: 10.1021/bc060316h. Epub 2007 Mar 23.
Identification of a tumor angiogenesis specific ligand would allow targeting of tumor vasculature. Lipidic vehicles can be used to deliver therapeutic agents for treatment of disease or contrast agents for molecular imaging. A targeting ligand would allow specific delivery of such formulations to angiogenic sites, thereby reducing side effects and gaining efficiency. Anginex, a synthetic 33-mer angiostatic peptide, has been described to home angiogenically activated endothelium, suggesting an ideal candidate as targeting ligand. To investigate this application of anginex, fluorescently labeled paramagnetic liposomes were conjugated with anginex. Using phase contrast and fluorescence microscopy as well as magnetic resonance imaging (MRI), we demonstrate that anginex-conjugated liposomes bind specifically to activated endothelial cells, suggesting application as an angiogenesis targeting agent for molecular targeting and molecular imaging of angiogenesis-dependent disease.
鉴定肿瘤血管生成特异性配体将有助于靶向肿瘤血管系统。脂质载体可用于递送治疗疾病的治疗剂或用于分子成像的造影剂。靶向配体可使此类制剂特异性递送至血管生成部位，从而减少副作用并提高效率。血管抑制素（Anginex）是一种合成的33肽血管抑制肽，已被描述可归巢至血管生成激活的内皮细胞，提示其是作为靶向配体的理想候选物。为了研究血管抑制素的这种应用，将荧光标记的顺磁性脂质体与血管抑制素偶联。使用相差显微镜和荧光显微镜以及磁共振成像（MRI），我们证明血管抑制素偶联的脂质体可特异性结合激活的内皮细胞，提示其可作为血管生成靶向剂用于血管生成依赖性疾病的分子靶向和分子成像。
