Xie Jianwu, Shen Zhimin, Li King C P, Danthi Narasimhan
Molecular Imaging Laboratory, Clinical Center, National Institutes of Health, Bethesda, MD, USA.
Int J Nanomedicine. 2007;2(3):479-85.
Angiogenesis is an important process in cancer growth and metastasis. During the tumor angiogenic process, endothelial cells express various cell surface receptors which can be utilized for molecular imaging and targeted drug delivery. One such protein receptor of interest is the integrin alphav beta3. Our group is involved in the development of molecular imaging probes and drug delivery systems targeting alphav beta3. Based on extensive lead optimization study with the integrin antagonist compounds, we have developed a new generation of integrin alphav beta3 compound (IA) which has superior binding affinity to alphav beta3. Utilizing this IA as a targeting agent, we have developed a novel integrin-targeted nanoparticle (ITNP) system for targ alphav beta3 was observed. These ITNPs also were rapidly taken up by cells that express alphav beta3. The ITNPs accumulated in the angiogenic vessels, after systemic administration in a murine squamous cell carcinoma model. This novel intergrin targeted ITNP platform will likely have an application in targeted delivery of drugs and genes in vivo and can also be used for molecular imaging.
血管生成是癌症生长和转移过程中的一个重要过程。在肿瘤血管生成过程中，内皮细胞表达各种细胞表面受体，这些受体可用于分子成像和靶向药物递送。一种这样的感兴趣的蛋白质受体是整合素αvβ3。我们的团队参与了针对αvβ3的分子成像探针和药物递送系统的开发。基于对整合素拮抗剂化合物的广泛先导优化研究，我们开发了新一代整合素αvβ3化合物（IA），它对αvβ3具有优异的结合亲和力。利用这种IA作为靶向剂，我们开发了一种新型的整合素靶向纳米颗粒（ITNP）系统用于靶向αvβ3。观察到这些ITNP也被表达αvβ3的细胞迅速摄取。在小鼠鳞状细胞癌模型中进行全身给药后，ITNP在血管生成血管中积累。这种新型的整合素靶向ITNP平台可能在体内药物和基因的靶向递送中具有应用价值，并且还可用于分子成像。
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