ArticleBioconjugate chemistry2012
Efficient method for site-specific 18F-labeling of biomolecules using the rapid condensation reaction between 2-cyanobenzothiazole and cysteine.
Article in Bioconjugate chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed.
- Toward Precision Bioconjugation: Chemical Strategies for Site-Selective Cysteine Conjugation.Precision chemistry · 2026Review
- Bioorthogonal Chemistry in Biomolecule Quantification: A Review of Reactions and Strategies.Chemistry (Weinheim an der Bergstrasse, Germany) · 2026Review
- From molecules to medicine: thiol selective bioconjugation in synthesis of diagnostic and therapeutic radiopharmaceuticals.Theranostics · 2024Review
- Click chemistry approaches for developing carbonic anhydrase inhibitors and their applications.Journal of enzyme inhibition and medicinal chemistry · 2023Review
- Exploiting Protein N-Terminus for Site-Specific Bioconjugation.Molecules (Basel, Switzerland) · 2021Review
- Single-Molecule Observation of Intermediates in Bioorthogonal 2-Cyanobenzothiazole Chemistry.Angewandte Chemie (International ed. in English) · 2020Article
- Introducing charge tagChemical science · 2020Article
- Recent Advances in Bioorthogonal Click Chemistry for Efficient Synthesis of Radiotracers and Radiopharmaceuticals.Molecules (Basel, Switzerland) · 2019Review
- A Flexible Synthesis ofMolecules (Basel, Switzerland) · 2018Article
- Computation-Guided Rational Design of a Peptide Motif That Reacts with Cyanobenzothiazoles via Internal Cysteine-Lysine Relay.The Journal of organic chemistry · 2018Article
- Review
- Targeting the N terminus for site-selective protein modification.Nature chemical biology · 2017Review
- Preclinical validations of [EJNMMI radiopharmacy and chemistry · 2017Article
- Mechanistic study of CBT-Cys click reaction and its application for identifying bioactive N-terminal cysteine peptides in amniotic fluid.Chemical science · 2017Article
- Click Chemistry and Radiochemistry: The First 10 Years.Bioconjugate chemistry · 2016Review
- Site-Specific Radiofluorination of Biomolecules with 8-[(18)F]-Fluorooctanoic Acid Catalyzed by Lipoic Acid Ligase.ACS chemical biology · 2016Article
- Comparison of two site-specifically (18)F-labeled affibodies for PET imaging of EGFR positive tumors.Molecular pharmaceutics · 2014Article
- Positron emission tomography imaging of drug-induced tumor apoptosis with a caspase-triggered nanoaggregation probe.Angewandte Chemie (International ed. in English) · 2013Article
- Enhanced aqueous Suzuki-Miyaura coupling allows site-specific polypeptide 18F-labeling.Journal of the American Chemical Society · 2013Article
- Strategy for dual-analyte luciferin imaging: in vivo bioluminescence detection of hydrogen peroxide and caspase activity in a murine model of acute inflammation.Journal of the American Chemical Society · 2013Article
Corrections and comments
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Authors and funding
7 authors.
Funding
Abstract
An efficient method based on a rapid condensation reaction between 2-cyanobenzothiazole (CBT) and cysteine has been developed for (18)F-labeling of N-terminal cysteine-bearing peptides and proteins. An (18)F-labeled dimeric cRGD ([(18)F]CBTRGD(2)) has been synthesized with an excellent radiochemical yield (92% based on radio-HPLC conversion, 80% decay-corrected, and isolated yield) and radiochemical purity (>99%) under mild conditions using (18)F-CBT, and shown good in vivo tumor targeting efficiency for PET imaging. The labeling strategy was also applied to the site-specific (18)F-labeling of a protein, Renilla lucifierase (RLuc8) with a cysteine residue at its N-terminus. The protein labeling was achieved with 12% of decay-corrected radiochemical yield and more than 99% radiochemical purity. This strategy should provide a general approach for efficient and site-specific (18)F-labeling of various peptides and proteins for in vivo molecular imaging applications.
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