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MR Molecular Imaging of Prostate Cancer with a Small Molecular CLT1 Peptide Targeted Contrast Agent
Published on: September 3, 2013
GRPR-selective PET imaging of prostate cancer using [(18)F]-lanthionine-bombesin analogs
G Carlucci1, A Kuipers2, H J K Ananias3
1Department of Urology, University Medical Center Groningen, University of Groningen, Groningen, The Netherlands; Department of Nuclear Medicine and Molecular Imaging, University Medical Center Groningen, University of Groningen, Groningen, The Netherlands.
Abstract:
The gastrin-releasing peptide receptor (GRPR) is overexpressed in a variety of human malignancies, including prostate cancer. Bombesin (BBN) is a 14 amino acids peptide that selectively binds to GRPR. In this study, we developed two novel Al(18)F-labeled lanthionine-stabilized BBN analogs, designated Al(18)F-NOTA-4,7-lanthionine-BBN and Al(18)F-NOTA-2,6-lanthionine-BBN, for positron emission tomography (PET) imaging of GRPR expression using xenograft prostate cancer models. (Methyl)lanthionine-stabilized 4,7-lanthionine-BBN and 2,6-lanthionine-BBN analogs were conjugated with a NOTA chelator and radiolabeled with Al(18)F using the aluminum fluoride strategy. Al(18)F-NOTA-4,7-lanthionine-BBN and Al(18)F-NOTA-2,6-lanthionine-BBN was labeled with Al(18)F with good radiochemical yield and specific activity>30 GBq/μmol for both radiotracers. The logD values measured for Al(18)F-NOTA-4,7-lanthionine-BBN and Al(18)F-NOTA-2,6-lanthionine-BBN were -2.14 ± 0.14 and -2.34 ± 0.15, respectively. In athymic nude PC-3 xenografts, at 120 min post injection (p.i.), the uptake of Al(18)F-NOTA-4,7-lanthionine-BBN and Al(18)F-NOTA-2,6-lanthionine-BBN in prostate cancer (PC-3) mouse models was 0.82 ± 0.23% ID/g and 1.40 ± 0.81% ID/g, respectively. An excess of unlabeled ɛ-aminocaproic acid-BBN(7-14) (300-fold) was co-injected to assess GRPR binding specificity. Tumor uptake of Al(18)F-NOTA-4,7-lanthionine-BBN and Al(18)F-NOTA-2,6-lanthionine-BBN in PC-3 tumors was evaluated by microPET (μPET) imaging at 30, 60 and 120 min p.i. Blocking studies showed decreased uptake in PC-3 bearing mice. Stabilized 4,7-lanthionine-BBN and 2,6-lanthionine-BBN peptides were rapidly and successfully labeled with (18)F. Both tracers may have potential for GRPR-positive tumor imaging.
Insights
Two new Al(18)F-labeled bombesin (BBN) analogs targeting the gastrin-releasing peptide receptor (GRPR) show potential for PET imaging of prostate cancer. These radiotracers demonstrated successful labeling and specific uptake in GRPR-positive tumors.
Area of Science:
- Nuclear Medicine
- Radiochemistry
- Oncology
Background:
- Gastrin-releasing peptide receptor (GRPR) is overexpressed in various human cancers, including prostate cancer.
- Bombesin (BBN) is a peptide that selectively binds to GRPR, making it a target for cancer imaging.
- Developing novel radiotracers for Positron Emission Tomography (PET) is crucial for visualizing GRPR expression in vivo.
Purpose of the Study:
- To develop and evaluate novel Al(18)F-labeled lanthionine-stabilized BBN analogs for PET imaging of GRPR.
- To assess the feasibility of using these tracers for visualizing GRPR-positive prostate cancer xenografts in mouse models.
Main Methods:
- Synthesis of lanthionine-stabilized BBN analogs conjugated with a NOTA chelator.
- Radiolabeling of analogs with Al(18)F using the aluminum fluoride strategy.
- Evaluation of radiochemical yield, specific activity, and logD values.
- In vivo microPET imaging in PC-3 xenograft mouse models, including blocking studies to confirm GRPR specificity.
Main Results:
- Two novel Al(18)F-labeled tracers, Al(18)F-NOTA-4,7-lanthionine-BBN and Al(18)F-NOTA-2,6-lanthionine-BBN, were successfully synthesized.
- Both radiotracers exhibited good radiochemical yield and high specific activity (>30 GBq/μmol).
- In vivo studies showed specific uptake of the tracers in PC-3 tumors, which was reduced by co-injection of unlabeled BBN, confirming GRPR targeting.
Conclusions:
- Lanthionine-stabilized BBN analogs can be efficiently labeled with Al(18)F.
- The developed Al(18)F-labeled tracers demonstrate potential for non-invasive PET imaging of GRPR-positive tumors.
- These novel radiotracers may aid in the diagnosis and management of prostate cancer.
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