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标题：66Ga-PET-imaging of GRPR-expression in prostate cancer: production and characterization of [66Ga]Ga-NOTA-PEG2-RM26
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作者：Sara S. Rinne ; Ayman Abouzayed ; Katherine Gagnon 等
期刊名称：Scientific Reports
电子版ISSN：2045-2322
出版年度：2021
卷号：11
期号：1
页码：3631
DOI：10.1038/s41598-021-82995-7
出版社：Springer Nature
摘要：Abstract Molecular imaging of the gastrin-releasing peptide receptor (GRPR) could improve patient management in prostate cancer. This study aimed to produce gallium-66 (T ½ = 9.5 h) suitable for radiolabeling, and investigate the imaging properties of gallium-66 labeled GRPR-antagonist NOTA-PEG 2 -RM26 for later-time point PET-imaging of GRPR expression. Gallium-66 was cyclotron-produced using a liquid target, and enriched [ 66 Zn]Zn(NO 3 ) 2 . In vitro, [ 66 Ga]Ga-NOTA-PEG 2 -RM26 was characterized in GRPR-expressing PC-3 prostate cancer cells. In vivo, specificity test and biodistribution studies were performed 3 h and 22 h pi in PC-3 xenografted mice. microPET/MR was performed 3 h and 22 h pi. Biodistribution of [ 66 Ga]Ga-NOTA-PEG 2 -RM26 was compared with [ 68 Ga]Ga-NOTA-PEG 2 -RM26 3 h pi. [ 66 Ga]Ga-NOTA-PEG 2 -RM26 was successfully prepared with preserved binding specificity and high affinity towards GRPR. [ 66 Ga]Ga-NOTA-PEG 2 -RM26 cleared rapidly from blood via kidneys. Tumor uptake was GRPR-specific and exceeded normal organ uptake. Normal tissue clearance was limited, resulting in no improvement of tumor-to-organ ratios with time. Tumors could be clearly visualized using microPET/MR. Gallium-66 was successfully produced and [ 66 Ga]Ga-NOTA-PEG 2 -RM26 was able to clearly visualize GRPR-expression both shortly after injection and on the next day using PET. However, delayed imaging did not improve contrast for Ga-labeled NOTA-PEG 2 -RM26.
其他摘要：Abstract Molecular imaging of the gastrin-releasing peptide receptor (GRPR) could improve patient management in prostate cancer. This study aimed to produce gallium-66 (T ½ = 9.5 h) suitable for radiolabeling, and investigate the imaging properties of gallium-66 labeled GRPR-antagonist NOTA-PEG 2 -RM26 for later-time point PET-imaging of GRPR expression. Gallium-66 was cyclotron-produced using a liquid target, and enriched [ 66 Zn]Zn(NO 3 ) 2 . In vitro, [ 66 Ga]Ga-NOTA-PEG 2 -RM26 was characterized in GRPR-expressing PC-3 prostate cancer cells. In vivo, specificity test and biodistribution studies were performed 3 h and 22 h pi in PC-3 xenografted mice. microPET/MR was performed 3 h and 22 h pi. Biodistribution of [ 66 Ga]Ga-NOTA-PEG 2 -RM26 was compared with [ 68 Ga]Ga-NOTA-PEG 2 -RM26 3 h pi. [ 66 Ga]Ga-NOTA-PEG 2 -RM26 was successfully prepared with preserved binding specificity and high affinity towards GRPR. [ 66 Ga]Ga-NOTA-PEG 2 -RM26 cleared rapidly from blood via kidneys. Tumor uptake was GRPR-specific and exceeded normal organ uptake. Normal tissue clearance was limited, resulting in no improvement of tumor-to-organ ratios with time. Tumors could be clearly visualized using microPET/MR. Gallium-66 was successfully produced and [ 66 Ga]Ga-NOTA-PEG 2 -RM26 was able to clearly visualize GRPR-expression both shortly after injection and on the next day using PET. However, delayed imaging did not improve contrast for Ga-labeled NOTA-PEG 2 -RM26.