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68-Ga-labeled NODAGA-RGD-BBN heterodimer peptide as a novel radiotracer for dual integrin and GRPR-targeted tumor imaging
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| N. Amraee, B. Alirezapour, M. Hosntalab, A. Hadadi, H. Yousefnia |
| Radiation Application Research School, Nuclear Science and Technology Research Institute (NSTRI), Tehran, Iran , balirezapour1358@gmail.com |
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Abstract: (768 Views) |
Background: Due to the excellent physical and biochemical characteristics of 68Ga, 68Ga-1,4,7-triazacy–clononane–glutaric acid– 4,7 acetic acid- arginyl-glycyl-aspartic acid- bombesin (68Ga-NODAGA-RGD-BBN) was prepared as a new positron emission tomography (PET) imaging agent, and afterward, the preclinical evaluation of this labeled peptide was studied. Materials and Methods: 68Ga radioisotope was extracted from a 68Ge/68Ga generator with high radionuclide, chemical and radiochemical purities. Then; the 68Ga-NODAGA-RGD-BBN radiolabeled complex was prepared at optimized conditions. The stability of the complex was evaluated in phosphate-buffered saline (PBS) for at least 2 h. Cell studies of the radiolabeled peptide were also assessed on the gastrin releasing peptide receptor (GRPR)-expressing cell line. Finally; the biodistribution and whole-body scan imaging study of 68Ga-NODAGA-RGD-BBN was studied in normal and tumor-bearing mice. Results: The biodistribution and whole-body scan imaging of the radiolabeled compound on GRPR-expressing tumor-bearing mice demonstrated the high uptake in the tumor site at all post-injection intervals. The biodistribution results also demonstrated the major excretion route of the complex is the urinary tract. Conclusions: 68Ga-NODAGA-RGD-BBN shows high potential for PET imaging of patients with GRPR-expressing tumors; however, more biological studies are still needed. |
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| Keywords: GRPR positive tumors, radiolabeling, heterodimer peptide, PET imaging. |
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Full-Text [PDF 831 kb]
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Type of Study: Original Research |
Subject:
Radiation Biology
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