Comprehensive Cancer Imaging Centre, Department of Surgery and Cancer, Hammersmith Campus, Imperial College London, Du Cane Road, London, W12 0NN, UK.
Dalton Trans. 2014 Apr 14;43(14):5535-45. doi: 10.1039/c3dt53095g. Epub 2014 Feb 18.
A series of new upconversion nanoparticles have been functionalised with tumour-targeting molecules and metal chelates, prepared following standard peptidic and thiol chemistry. The targeting strategy has been delivered via the αvβ3 integrin, which is a heterodimeric cell surface receptor that is up-regulated in a variety of cancers, such as melanoma and breast cancer. The well-known DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) motif allows coordination to the radionuclide (68)Ga. Radiolabelling experiments were optimised under relatively mild conditions, and are rare amongst nanoparticulate materials. In vivo application of these probes in mouse tumour models revealed their potential as specific cancer contrast agents for PET imaging.
一系列新的上转换纳米粒子已经通过肿瘤靶向分子和金属螯合物进行了功能化，这些靶向分子和金属螯合物是按照标准的肽和巯基化学方法制备的。该靶向策略是通过αvβ3 整合素来实现的，αvβ3 整合素是一种异二聚体细胞表面受体，在多种癌症中上调，如黑色素瘤和乳腺癌。众所周知的 DOTA（1,4,7,10-四氮杂环十二烷-1,4,7,10-四乙酸）基序允许与放射性核素（68）Ga 配位。在相对温和的条件下优化了放射性标记实验，这在纳米颗粒材料中很少见。这些探针在小鼠肿瘤模型中的体内应用揭示了它们作为 PET 成像特定癌症对比剂的潜力。
