ArticleBioconjugate chemistry2015
One-step (18)F labeling of non-peptidic bivalent integrin αvβ3 antagonist for cancer imaging.
Article in Bioconjugate chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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Who cites it
6 citing papers in PubMed, 15 citations in OpenAlex.
- Sortase-Mediated Site-Specific Conjugation to Prepare Fluorine-18-Labeled Nanobodies.Bioconjugate chemistry · 2024Article
- A Comprehensive Review of Non-Covalent Radiofluorination Approaches Using Aluminum [Molecules (Basel, Switzerland) · 2019Review
- Direct fluorine-18 labeling of heat-sensitive biomolecules for positron emission tomography imaging using the AlNature protocols · 2018Article
- AlTheranostics · 2017Article
- Small Molecule Radiopharmaceuticals - A Review of Current Approaches.Frontiers in medicine · 2016Review
- Pet Imaging and its Application in Cardiovascular Diseases.Methodist DeBakey cardiovascular journalReview
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Authors and funding
3 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A rapid one-step (18)F labeling reaction with fluoridealuminum complex, which is based on chelation chemistry, has received a surge of interest for (18)F radiolabeling of peptides. In this study, a non-peptidic bivalent integrin αvβ3 antagonist (bivalent-IA) was conjugated with 1,4,7-triazacyclononane-1,4-diiacetic acid (NODA). A novel (18)F labeled radiotracer, (18)F-bivalent-IA, was developed via one step (18)F-AlF/NODA chelation reaction in aqueous phase with high radiochemical yield (65-75%, decay corrected) and good specific activity (750-850 mCi/μmol). The tumor integrin targeting efficiency and in vivo pharmacokinetic profile of (18)F-bivalent-IA were evaluated in U-87 MG (integrin positive) and MDA-MB-231 (integrin negative) models by small-animal PET/CT scan followed by a biodistribution study. The PET/CT and ROI results showed high tumor uptake of (18)F-bivalent-IA in U-87 MG tumor-bearing mice from 5 to 120 min p.i. with good contrast, and the U-87 MG tumor uptake values (6.35 ± 0.67%ID/g, at 1 h p.i.) were 6 times higher than those of MDA-MB-231 tumor (1.05 ± 0.12%ID/g, at 1 h p.i.) (P < 0.0001) which correlated with the integrin αvβ3 expression in tumor tissues confirmed by immunohistochemistry. Co-injection of the (18)F-bivalent-IA with 6 nmol (6 μg) of nonradioactive bivalent-IA effectively blocked tumor uptake demonstrating the integrin αvβ3-specificity. In conclusion, the first (18)F labeled non-peptidic bivalent integrin αvβ3 targeting radiotracer, (18)F-bivalent-IA, was developed and proved to be a highly potent and specific PET radiopharmaceutical for noninvasive imaging of integrin αvβ3, which plays a critical role in tumor angiogenesis and metastasis.
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