scholarly journals Multivalent Bifunctional Chelator Scaffolds for Gallium-68 Based Positron Emission Tomography Imaging Probe Design: Signal Amplification via Multivalency

2011 ◽  
Vol 22 (8) ◽  
pp. 1650-1662 ◽  
Author(s):  
Ajay N. Singh ◽  
Wei Liu ◽  
Guiyang Hao ◽  
Amit Kumar ◽  
Anjali Gupta ◽  
...  
Keyword(s):  
Positron Emission Tomography ◽  
Signal Amplification ◽  
Positron Emission Tomography Imaging ◽  
Emission Tomography ◽  
Probe Design ◽  
Tomography Imaging ◽  
Imaging Probe ◽  
Bifunctional Chelator ◽  
Positron Emission ◽  
Gallium 68

A Uniquely Modified DKL-based Peptide Probe for Positron Emission Tomography Imaging

2019 ◽  
Vol 25 (1) ◽  
pp. 96-103
Author(s):  
Yi Liu ◽  
Zhengjie Wang ◽  
Xiang Li ◽  
Fei Kang ◽  
Xiaowei Ma ◽  
...  
Keyword(s):  
Positron Emission Tomography ◽  
Positron Emission Tomography Imaging ◽  
Emission Tomography ◽  
Tomography Imaging ◽  
Positron Emission ◽  
Imaging Results ◽  
Gallium 68 ◽  
Tumor Selective

Peptides containing the asparagine-glycine-arginine (NGR) motif can target the tumor neovascular biomarker CD13/aminopeptidase N receptor. D-K6L9 is a tumor-selective anti-cancer peptide. To improve the capacity of NGR peptides to target tumors, we joined the NGR and D-K6L9 peptides to form NKL. Next, we linked 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) to NKL and labeled it with gallium 68 (68Ga, t1/2 = 67.7 min) to form 68Ga-DOTA-NKL. This novel probe was characterized in vitro. 68Ga-DOTA-NKL was stable in phosphate buffered saline at room temperature and in human serum at 37°C. We determined that the uptake rate of 68Ga-DOTA-NKL in CD13 receptor-positive 22Rv1 tumor cells was 3.15% ± 0.04 after 2 h, and tested 68Ga-DOTA-NKL using positron emission tomography (PET)/computed tomography imaging in vivo. MicroPET imaging results revealed that 22Rv1 tumor uptake of 68Ga-DOTA-NKL was 8.69 ± 0.20, 6.61 ± 0.22, 3.85 ± 0.06, and 1.41 ± 0.23 percentage injected dose per gram of tissue (%ID/g) at 0.5, 1, 2, and 3 h postinjection (pi), respectively. The tumor-to-background contrast in the subcutaneous human prostate cancer 22Rv1 mouse model was 9.97 ± 1.90. The 68Ga-DOTA-NKL probe has combined tumor-targeting and tumor-selective properties, and may be used to diagnose CD13-positive tumors.

Catechol-Based Functionalizable Ligands for Gallium-68 Positron Emission Tomography Imaging

2020 ◽  
Vol 59 (17) ◽  
pp. 12025-12038
Author(s):  
M. Andrey Joaqui-Joaqui ◽  
Mukesh K. Pandey ◽  
Aditya Bansal ◽  
Mandapati V. Ramakrishnam Raju ◽  
Fiona Armstrong-Pavlik ◽  
...  
Keyword(s):  
Positron Emission Tomography ◽  
Positron Emission Tomography Imaging ◽  
Emission Tomography ◽  
Tomography Imaging ◽  
Positron Emission ◽  
Gallium 68
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