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

68Ga-labeled cyclic NGR peptide for microPET imaging of CD13 receptor expression.
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68Ga 标记的环状 NGR 肽,用于 CD13 受体表达的 microPET 成像。

DOI:
10.3390/molecules190811600
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发表时间:
2014-08-05
期刊:
Molecules (Basel, Switzerland)
影响因子:
--
通讯作者:
Wang J
Wang J
中科院分区:
其他
文献类型:
--
作者:
Shao Y;Liang W;Kang F;Yang W;Ma X;Li G;Zong S;Chen K;Wang J

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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 68Ga (t1/2 = 67.7 min). The resulting 68Ga-NOTA-G3-NGR peptide was subject to in vitro and in vivo characterization. The microPET imaging results revealed that the 68Ga-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 68Ga-NOTA-G3-NGR peptide has potential in the diagnosis of CD13-targeted tumor angiogenesis.
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