(68)Ga-Labeled Cyclic NGR Peptide for MicroPET Imaging of CD13 Receptor Expression

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-G(3)-NGR), and labeled NOTA-G(3)-NGR with (68)G...

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Detalles Bibliográficos
Autores principales: Shao, Yahui, Liang, Wansheng, Kang, Fei, Yang, Weidong, Ma, Xiaowei, Li, Guiyu, Zong, Shu, Chen, Kai, Wang, Jing
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2014
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271277/
https://www.ncbi.nlm.nih.gov/pubmed/25100253
http://dx.doi.org/10.3390/molecules190811600
Descripción
Sumario: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-G(3)-NGR), and labeled NOTA-G(3)-NGR with (68)Ga (t(1/2) = 67.7 min). The resulting (68)Ga-NOTA-G(3)-NGR peptide was subject to in vitro and in vivo characterization. The microPET imaging results revealed that the (68)Ga-NOTA-G(3)-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-G(3)-NGR peptide has potential in the diagnosis of CD13-targeted tumor angiogenesis.

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