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Region Hovedstaden - en del af Københavns Universitetshospital
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Preclinical Study on GRPR-Targeted (68)Ga-Probes for PET Imaging of Prostate Cancer

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  • Yao Sun
  • Xiaowei Ma
  • Zhe Zhang
  • Ziyan Sun
  • Mathias Loft
  • Bingbing Ding
  • Changhao Liu
  • Liying Xu
  • Meng Yang
  • Yuxin Jiang
  • Jianfeng Liu
  • Yuling Xiao
  • Zhen Cheng
  • Xuechuan Hong
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Gastrin-releasing peptide receptor (GRPR) targeted positron emission tomography (PET) is a highly promising approach for imaging of prostate cancer (PCa) in small animal models and patients. Developing a GRPR-targeted PET probe with excellent in vivo performance such as high tumor uptake, high contrast, and optimal pharmacokinetics is still very challenging. Herein, a novel bombesin (BBN) analogue (named SCH1) based on JMV594 peptide modified with an 8-amino octanoic acid spacer (AOC) was thus designed and conjugated with the metal chelator 1,4,7-triazacyclononane,1-glutaric acid-4,7-acetic acid (NODAGA). The resulting NODAGA-SCH1 was then radiolabeled with (68)Ga and evaluated for PET imaging of PCa. Compared with (68)Ga-NODAGA-JMV594 probe, (68)Ga-NODAGA-SCH1 exhibited excellent PET/CT imaging properties on PC-3 tumor-bearing nude mice, such as high tumor uptake (5.80 ± 0.42 vs 3.78 ± 0.28%ID/g, 2 h) and high tumor/muscle contrast (16.6 ± 1.50 vs 8.42 ± 0.61%ID/g, 2 h). Importantly, biodistribution data indicated a relatively similar accumulation of (68)Ga-NODAGA-SCH1 was observed in the liver (4.21 ± 0.42%ID/g) and kidney (3.41 ± 0.46%ID/g) suggesting that the clearance is through both the kidney and the liver. Overall, (68)Ga-NODAGA-SCH1 showed promising in vivo properties and is a promising candidate for translation into clinical PET-imaging of PCa patients.

OriginalsprogEngelsk
TidsskriftBioconjugate Chemistry
Vol/bind27
Udgave nummer8
Sider (fra-til)1857-64
Antal sider8
ISSN1043-1802
DOI
StatusUdgivet - 17 aug. 2016

ID: 49946762