用于CD13受体表达微PET成像的68Ga标记环状NGR肽

68Ga-labeled cyclic NGR peptide for microPET imaging of CD13 receptor expression.

作者信息

Shao Yahui, Liang Wansheng, Kang Fei, Yang Weidong, Ma Xiaowei, Li Guiyu, Zong Shu, Chen Kai, Wang Jing

机构信息

Department of Nuclear Medicine, Xijing Hospital, The Fourth Military Medical University, Xi'an 710032, China.

Department of Nuclear Medicine, Lanzhou General Hospital of Lanzhou Military Area Command, Lanzhou 730050, China.

出版信息

Molecules. 2014 Aug 5;19(8):11600-12. doi: 10.3390/molecules190811600.

Peptides containing the asparagines-glycine-arginine (NGR) motif have been identified as specific ligands binding to CD13/aminopeptidase N (APN) receptor, a tumor neovascular biomarker. In this study, we synthesized a novel NGR-containing peptide (NOTA-G3-NGR), and labeled NOTA-G3-NGR with (68)Ga (t1/2 = 67.7 min). The resulting (68)Ga-NOTA-G3-NGR peptide was subject to in vitro and in vivo characterization. The microPET imaging results revealed that the (68)Ga-NOTA-G3-NGR peptide exhibits rapid and specific tumor uptake, and high tumor-to-background contrast in a subcutaneous HT-1080 fibrosarcoma mouse model. We concluded that the (68)Ga-NOTA-G3-NGR peptide has potential in the diagnosis of CD13-targeted tumor angiogenesis.

含有天冬酰胺-甘氨酸-精氨酸（NGR）基序的肽已被鉴定为与肿瘤新生血管生物标志物CD13/氨肽酶N（APN）受体结合的特异性配体。在本研究中，我们合成了一种新型的含NGR肽（NOTA-G3-NGR），并用（68）Ga（半衰期=67.7分钟）对NOTA-G3-NGR进行标记。所得的（68）Ga-NOTA-G3-NGR肽进行了体外和体内表征。微型正电子发射断层扫描（microPET）成像结果显示，在皮下HT-1080纤维肉瘤小鼠模型中，（68）Ga-NOTA-G3-NGR肽表现出快速且特异性的肿瘤摄取以及高肿瘤与背景对比度。我们得出结论，（68）Ga-NOTA-G3-NGR肽在诊断CD13靶向的肿瘤血管生成方面具有潜力。