Biodistribution and evaluation of ¹³¹I-labeled neuropilin-binding peptide for targeted tumor imaging

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• 作者：Ping Dong ; Huawei Cai ; Lihong Chen ; Yalun Li ; Cen Yuan ; Xiaoai Wu ; Guohua Shen ; Huijun Zhou ; Wenjie Zhang and Lin Li
• 刊名：Contrast Media & Molecular Imaging
• 出版年：2016
• 出版时间：November/December 2016
• 年：2016
• 卷：11
• 期：6
• 页码：467-474
• 全文大小：586K
• ISSN：1555-4317

文摘

Neuropilin-1 (NRP-1) is overexpressed in several kinds of cancer cell and contributes to tumor aggressiveness. Recently, the arginine/lysine-rich peptide with C-terminal motifs (R/K)XX(R/K) indicated promising penetrating and transporting capability into NRP-1 positive cancer cells. In the present study, we describe a ¹³¹I-labeled C-end rule motif peptide conjugate, Tyr–tLyp-1, for NRP-1 positive tumor targeting and imaging properties. Briefly, a truncated Lyp-1 peptide was designed to expose its C-end motif and conjugated to tyrosine for radiolabeling after structural modification. The peptide indicated specific binding to A549 cancer cells at 2 μM concentration, and its binding was dependent on NRP-1 expression and could be inhibited by other NRP-1-binding peptides. In vivo imaging of ¹³¹I-labeled Tyr–tLyp-1peptide showed that a subcutaneous A549 xenograft tumor could be visualized using a SPECT/CT scanner. The tumor uptake of ¹³¹I-Tyr–tLyp-1 was 4.77 times higher than the uptake in muscles by SPECT/CT software quantification at 6 h post injection. Together, this study indicated that truncated Lyp-1 peptide could specifically localize in NRP-1 positive tumors and successfully mediate the ¹³¹I radionuclide diagnosis, indicating promising targeted imaging capability for NRP-1 positive tumors. Copyright