@article{oai:kanazawa-u.repo.nii.ac.jp:00058970,
 author = {三代, 憲司 and 淵上, 剛志 and 柴, 和弘 and 絹谷, 清剛 and 小川, 数馬 and Echigo, Hiroaki and Mishiro, Kenji and Fuchigami, Takeshi and Shiba, Kazuhiro and Kinuya, Seigo and Ogawa, Kazuma},
 issue = {20},
 journal = {Molecules},
 month = {},
 note = {We recently developed125I-and211At-labeled monomer RGD peptides using a novel radi-olabeling method. Both labeled peptides showed high accumulation in the tumor and exhibited similar biodistribution, demonstrating their usefulness for radiotheranostics. This study applied the labeling method to a dimer RGD peptide with the aim of gaining higher accumulation in tumor tissues based on improved affinity with αvβ3 integrin. We synthesized an iodine-introduced dimer RGD peptide, E[c(RGDfK)] (6), and an 125/131 I-labeled dimer RGD peptide, E[c(RGDfK)]{[125/131I]c[RGDf(4-I)K]} ([125/131I]6), and evaluated them as a preliminary step to the synthesis of an211At-labeled dimer RGD peptide. The affinity of 6 for αvβ3 integrin was higher than that of a monomer RGD peptide. In the biodistribution experiment at 4 h postinjection, the accumulation of [125I]6 (4.12 ± 0.42% ID/g) in the tumor was significantly increased compared with that of125I-labeled monomer RGD peptide (2.93 ± 0.08% ID/g). Moreover, the accumulation of [125I]6 in the tumor was greatly inhibited by co-injection of an excess RGD peptide. However, a single injection of [131I]6 (11.1 MBq) did not inhibit tumor growth in tumor-bearing mice. We expect that the labeling method for targeted alpha therapy with211At using a dimer RGD peptide could prove useful in future clinical applications. © 2021 by the authors. Licensee MDPI, Basel, Switzerland., CC-BY 4.0, 金沢大学疾患モデル総合研究センター},
 title = {Synthesis and evaluation of a dimeric rgd peptide as a preliminary study for radiotheranostics with radiohalogens},
 volume = {26},
 year = {2021}
}