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

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 ¹³¹ I-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 ¹³¹ I-labeled Tyr-tLyp-1peptide showed that a subcutaneous A549 xenograft tumor could be visualized using a SPECT/CT scanner. The tumor uptake of ¹³¹ I-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 ¹³¹ I radionuclide diagnosis, indicating promising targeted imaging capability for NRP-1 positive tumors. Copyright © 2016 John Wiley & Sons, Ltd.