ArticleAmerican journal of nuclear medicine and molecular imaging2013
One-step and one-pot-two-step radiosynthesis of cyclo-RGD-(18)F-aryltrifluoroborate conjugates for functional imaging.
Article in American journal of nuclear medicine and molecular imaging, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
14 citing papers in PubMed, 26 citations in OpenAlex.
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- Review
- Dual PET and Near-Infrared Fluorescence Imaging Probes as Tools for Imaging in Oncology.AJR. American journal of roentgenology · 2016Review
- Small Molecule Radiopharmaceuticals - A Review of Current Approaches.Frontiers in medicine · 2016Review
- 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
- Impact of multiple negative charges on blood clearance and biodistribution characteristics of 99mTc-labeled dimeric cyclic RGD peptides.Bioconjugate chemistry · 2014Article
- 18F-labeling using click cycloadditions.BioMed research international · 2014Review
- (99m)Tc-Galacto-RGD2: a novel 99mTc-labeled cyclic RGD peptide dimer useful for tumor imaging.Molecular pharmaceutics · 2013Article
- Recent trends in bioorthogonal click-radiolabeling reactions using fluorine-18.Molecules (Basel, Switzerland) · 2013Review
- Radiofluorination using aluminum-fluoride (Al18F).EJNMMI research · 2013Article
- "Kit like" (18)F labeling method for synthesis of RGD peptide-based PET probes.American journal of nuclear medicine and molecular imaging · 2013Article
- Multimodality imaging of RNA interference.Current medicinal chemistry · 2013Review
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Arylboronates capture aqueous (18)F-fluoride in one step to afford a highly polar (18)F-labeled aryltrifluoroborate anion ((18)F-ArBF(3) (-)) that clears rapidly in vivo. To date however, there is little data to show that a ligand labeled with a prosthetic (18)F-ArBF(3) (-) will provide functional images. RGD, a high-affinity ligand for integrins that are present on the cell surface of numerous tumors, has been labeled in many formats with many different radionuclides, and as such represents a well-established ligand that can be used to evaluate new labeling methods. Herein we have labeled RGD with a prosthetic (18)F-ArBF(3) (-) via two approaches for the first time: 1) a RGD-boronate bioconjugate is directly labeled in one step and 2) an alkyne-modified arylborimidine is first converted to the corresponding (18)F-ArBF(3) (-) which is then conjugated to an RGD-azide via Cu(+)-mediated [2+3] dipolar cycloaddition in one pot over two steps. RGD-(18)F-ArBF(3) (-) bionconjugates were produced in reasonable radiochemical yields using low amounts of (18)F-fluoride anion (10-50 mCi). Despite relatively low specific activities, good tumor images are revealed in each case.
Indexed as
Identifiers
23342300PMC3545361W1501026787What OpenQuestion holds
Registered trials
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.