ArticleBioconjugate chemistry2009
A novel method for direct site-specific radiolabeling of peptides using [18F]FDG.
Article in Bioconjugate chemistry, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
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Who cites it
29 citing papers in PubMed, 83 citations in OpenAlex.
- Enhancing theranostic potential of anti-mesothelin sdAb through site-specific labeling at a unique conserved lysine by molecular engineering.EJNMMI radiopharmacy and chemistry · 2025Article
- Innovative Peptide Bioconjugation Chemistry with Radionuclides: Beyond Classical Click Chemistry.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Article
- Chemoenzymatic Syntheses of Fluorine-18-Labeled Disaccharides from [Journal of the American Chemical Society · 2023Article
- Application of Metabolic Reprogramming to Cancer Imaging and Diagnosis.International journal of molecular sciences · 2022Review
- Sweetening Pharmaceutical Radiochemistry byPharmaceuticals (Basel, Switzerland) · 2021Review
- Targeting Prostate-Specific Membrane Antigen (PSMA) with F-18-Labeled Compounds: the Influence of Prosthetic Groups on Tumor Uptake and Clearance Profile.Molecular imaging and biology · 2017Article
- Solid-phase synthesis and fluorine-18 radiolabeling of cycloRGDyK.Organic & biomolecular chemistry · 2016Article
- A reactivity-based [Chemical science · 2016Article
- Caged [(18)F]FDG Glycosylamines for Imaging Acidic Tumor Microenvironments Using Positron Emission Tomography.Bioconjugate chemistry · 2016Article
- Radiolabeled cyclic RGD peptides as radiotracers for tumor imaging.Biophysics reports · 2016Review
- Radiolabeled Cyclic RGD Peptide Bioconjugates as Radiotracers Targeting Multiple Integrins.Bioconjugate chemistry · 2015Review
- The use ofACS central science · 2015Article
- One-pot two-step radiosynthesis of a new (18)F-labeled thiol reactive prosthetic group and its conjugate for insulinoma imaging.Molecular pharmaceutics · 2014Article
- Using 5-deoxy-5-[18F]fluororibose to glycosylate peptides for positron emission tomography.Nature protocols · 2014Article
- Sweetening pharmaceutical radiochemistry by (18)f-fluoroglycosylation: a short review.BioMed research international · 2014Review
- A one-pot enzymatic approach to the O-fluoroglucoside of N-methylanthranilate.Bioorganic & medicinal chemistry · 2013Article
- One-step (18)F-labeling of peptides for positron emission tomography imaging using the SiFA methodology.Nature protocols · 2012Article
- Site-selective glycosylation of hemoglobin with variable molecular weight oligosaccharides: potential alternative to PEGylation.Journal of the American Chemical Society · 2012Article
- Optimized labeling of NOTA-conjugated octreotide with F-18.Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine · 2012Article
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Authors and funding
9 authors at 2 institutions in 2 countries.
Funding
Abstract
We have used the well-accepted and easily available 2-[(18)F]fluoro-2-deoxyglucose ([(18)F]FDG) positron emission tomography (PET) tracer as a prosthetic group for synthesis of (18)F-labeled peptides. We herein report the synthesis of [(18)F]FDG-RGD ((18)F labeled linear RGD) and [(18)F]FDG-cyclo(RGD(D)YK) ((18)F labeled cyclic RGD) as examples of the use of [(18)F]FDG. We have successfully prepared [(18)F]FDG-RGD and [(18)F]FDG-cyclo(RGD(D)YK) in 27.5% and 41% radiochemical yields (decay corrected) respectively. The receptor binding affinity study of FDG-cyclo(RGD(D)YK) for integrin alpha(v)beta(3), using alpha(v)beta(3) positive U87MG cells confirmed a competitive displacement with (125)I-echistatin as a radioligand. The IC(50) value for FDG-cyclo(RGD(D)YK) was determined to be 0.67 +/- 0.19 muM. High-contrast small animal PET images with relatively moderate tumor uptake were observed for [(18)F]FDG-RGD and [(18)F]FDG-cyclo(RGD(D)YK) as PET probes in xenograft models expressing alpha(v)beta(3) integrin. In conclusion, we have successfully used [(18)F]FDG as a prosthetic group to prepare (18)F]FDG-RGD and [(18)F]FDG-cyclic[RGD(D)YK] based on a simple one-step radiosynthesis. The one-step radiosynthesis methodology consists of chemoselective oxime formation between an aminooxy-functionalized peptide and [(18)F]FDG. The results have implications for radiolabeling of other macromolecules and would lead to a very simple strategy for routine preclinical and clinical use.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.