Evaluation of a Cu-64-labeled 1,4,7-triazacyclononane, 1-glutaric acid-4,7 acetic acid (NODAGA)-galactose-bombesin analogue as a PET imaging probe in a gastrin-releasing peptide receptor-expressing prostate cancer xenograft model
- Authors
- Kim, Min Hwan; Park, Ji Ae; Woo, Sang-Keun; Lee, Kyo Chul; An, Gwang Il; Kim, Byoung Soo; Kim, Kwang Il; Lee, Tae Sup; Kim, Chan Wha; Kim, Kyeong Min; Kang, Joo Hyun; Lee, Yong Jin
- Issue Date
- 3월-2015
- Publisher
- SPANDIDOS PUBL LTD
- Keywords
- bombesin; Cu-64; positron emission tomography; prostate cancer; radiopharmaceuticals
- Citation
- INTERNATIONAL JOURNAL OF ONCOLOGY, v.46, no.3, pp.1159 - 1168
- Indexed
- SCIE
SCOPUS
- Journal Title
- INTERNATIONAL JOURNAL OF ONCOLOGY
- Volume
- 46
- Number
- 3
- Start Page
- 1159
- End Page
- 1168
- URI
- https://scholar.korea.ac.kr/handle/2021.sw.korea/94346
- DOI
- 10.3892/ijo.2015.2832
- ISSN
- 1019-6439
- Abstract
- Gastrin-releasing peptide receptor (GRPR) is overexpressed by a variety of human tumors and in particular, identified to be upregulated in prostate cancers. The current study aimed to develop clinically translatable BBN analogue-based radioligands for positron emission tomography (PET) of GRPR-positive tumors. We developed radiolabeled BBN analogues and modified radiolabeled galacto-BBN analogues and then investigated their tumor-targeting efficacy in vivo. The chelator 1,4,7-triazacyclononane, 1-glutaric acid-4,7 acetic acid (NODAGA) was used to radiolabel the peptides with Cu-64. The peptides were evaluated by measuring cell-based receptor-binding affinities. Biodistribution experiments and small animal imaging using PET were performed in nude mice bearing subcutaneous PC3 human prostate cancer xenografts. The conjugates were radiolabeled with yields >99%. The stability assay showed that [Cu-64] NODAGA-BBN and [Cu-64]NODAGA-galacto-BBN remained stable in both human and mouse serum for 1 h at 37 degrees C. PET images of PC3 tumor-bearing nude mice were acquired at 1, 3, 24, 48 and 72 h after injection. [64Cu]NODAGA-galacto-BBN showed retention in tumors for 72 h, low liver uptake, and rapid renal clearance. PET imaging results were also confirmed by biodistrubution 1 and 3 h after injection. [Cu-64]NODAGA-BBN and [Cu-64]NODAGA-galacto-BBN are promising new PET probes for GRPR-positive prostate cancer.
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Collections - College of Life Sciences and Biotechnology > Division of Life Sciences > 1. Journal Articles
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