title: Biodistribution and evaluation of131I-labeled neuropilin-binding peptide for targeted tumor imaging.
abstract: 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 a131I-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 of131I-labeled Tyr-tLyp-1peptide showed that a subcutaneous A549 xenograft tumor could be visualized using a SPECT/CT scanner. The tumor uptake of131I-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 the131I radionuclide diagnosis, indicating promising targeted imaging capability for NRP-1 positive tumors. Copyright © 2016 John Wiley & Sons, Ltd.
authors.affiliation: Department of Nuclear Medicine, West China Hospital, Sichuan University, Chengdu, 610041, People's Republic of China.
authors.forename: Ping
authors.initials: P
authors.lastname: Dong
authors.affiliation: Department of Nuclear Medicine, West China Hospital, Sichuan University, Chengdu, 610041, People's Republic of China.
authors.forename: Huawei
authors.initials: H
authors.lastname: Cai
authors.affiliation: Department of Biochemistry and Molecular Biology, West China School of Preclinical and Forensic Medicine, Sichuan University, Chengdu, 610041, People's Republic of China.
authors.forename: Lihong
authors.initials: L
authors.lastname: Chen
authors.affiliation: Department of Respiratory Medicine, West China Hospital, Sichuan University, Chengdu, 610041, People's Republic of China.
authors.forename: Yalun
authors.initials: Y
authors.lastname: Li
authors.affiliation: Department of Nuclear Medicine, West China Hospital, Sichuan University, Chengdu, 610041, People's Republic of China.
authors.forename: Cen
authors.initials: C
authors.lastname: Yuan
authors.affiliation: Department of Nuclear Medicine, West China Hospital, Sichuan University, Chengdu, 610041, People's Republic of China.
authors.forename: Xiaoai
authors.initials: X
authors.lastname: Wu
authors.affiliation: Department of Nuclear Medicine, West China Hospital, Sichuan University, Chengdu, 610041, People's Republic of China.
authors.forename: Guohua
authors.initials: G
authors.lastname: Shen
authors.affiliation: Department of Nuclear Medicine, West China Hospital, Sichuan University, Chengdu, 610041, People's Republic of China.
authors.forename: Huijun
authors.initials: H
authors.lastname: Zhou
authors.affiliation: Department of Nuclear Medicine, West China Hospital, Sichuan University, Chengdu, 610041, People's Republic of China.
authors.forename: Wenjie
authors.initials: W
authors.lastname: Zhang
authors.affiliation: Department of Nuclear Medicine, West China Hospital, Sichuan University, Chengdu, 610041, People's Republic of China.
authors.forename: Lin
authors.initials: L
authors.lastname: Li
mesh_terms: D000072283:A549 Cells; D006801:Humans; D007457:Iodine Radioisotopes; D057054:Molecular Imaging / Q000379:methods*; D009369:Neoplasms / Q000000981:diagnostic imaging*; D039942:Neuropilin-1 / Q000032:analysis* / Q000378:metabolism; D010456:Peptides, Cyclic / Q000378:metabolism; D011877:Radionuclide Imaging / Q000379:methods; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics; D000072098:Single Photon Emission Computed Tomography Computed Tomography; D014018:Tissue Distribution
chemical_list: D007457:Iodine Radioisotopes; C533969:LyP-1 peptide; D010456:Peptides, Cyclic; D019275:Radiopharmaceuticals; D039942:Neuropilin-1
keywords: C-end rule motif peptide; SPECT/CT; Tyr-tLyp-1; neuropilin-1