ArticleEJNMMI research2017
Simple, mild, one-step labelling of proteins with gallium-68 using a tris(hydroxypyridinone) bifunctional chelator: a
Article in EJNMMI research, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 31 citations in OpenAlex.
- EfficientInternational journal of molecular sciences · 2026Article
- Synthesis, radiolabeling, and biodistribution evaluation of novel hyperbranched polyglycerols-based radiotracers for targeting PSMA in prostate cancer.Iranian journal of basic medical sciences · 2026Article
- Article
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- The Chemical Scaffold of Theranostic Radiopharmaceuticals: Radionuclide, Bifunctional Chelator, and Pharmacokinetics Modifying Linker.Molecules (Basel, Switzerland) · 2022Review
- Hydroxypyridinones as a Very Promising Platform for Targeted Diagnostic and Therapeutic Radiopharmaceuticals.Molecules (Basel, Switzerland) · 2021Review
- State of the Art in Radiolabeling of Antibodies with Common and Uncommon Radiometals for Preclinical and Clinical Immuno-PET.Bioconjugate chemistry · 2021Article
- [Bioconjugate chemistry · 2021Article
- A simple strategy to reduce the salivary gland and kidney uptake of PSMA-targeting small molecule radiopharmaceuticals.European journal of nuclear medicine and molecular imaging · 2021Article
- NHS-Functionalized THP Derivative for Efficient Synthesis of Kit-Based Precursors forBiomedicines · 2021Article
- The chemical tool-kit for molecular imaging with radionuclides in the age of targeted and immune therapy.Cancer imaging : the official publication of the International Cancer Imaging Society · 2021Review
- ImmunoPET: Concept, Design, and Applications.Chemical reviews · 2020Review
- Targeted Radionuclide Therapy of Prostate Cancer-From Basic Research to Clinical Perspectives.Molecules (Basel, Switzerland) · 2020Review
- Manipulating the In Vivo Behaviour ofInternational journal of molecular sciences · 2020Article
- The effects of trace metal impurities on Ga-68-radiolabelling with a tris(3-hydroxy-1,6-dimethylpyridin-4-one) (THP) chelator.RSC advances · 2019Article
- Tuning the properties of tris(hydroxypyridinone) ligands: efficientDalton transactions (Cambridge, England : 2003) · 2019Article
- Antibody Fragment and Affibody ImmunoPET Imaging Agents: Radiolabelling Strategies and Applications.ChemMedChem · 2018Review
- Site-specific chelator-antibody conjugation for PET and SPECT imaging with radiometals.Drug discovery today. Technologies · 2018Review
- Theranostic radiopharmaceuticals: established agents in current use.The British journal of radiology · 2018Review
- In vitro cytotoxicity of Auger electron-emitting [Nuclear medicine and biologyArticle
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
backgroundLabelling proteins with gallium-68 using bifunctional chelators is often problematic because of unsuitably harsh labelling conditions such as low pH or high temperature and may entail post-labelling purification. To determine whether tris(hydroxypyridinone) (THP) bifunctional chelators offer a potential solution to this problem, we have evaluated the labelling and biodistribution of a THP conjugate with a new single-chain antibody against the prostate-specific membrane antigen (PSMA), an attractive target for staging prostate cancer (PCa). A single-chain variable fragment (scFv) of J591, a monoclonal antibody that recognises an external epitope of PSMA, was prepared in order to achieve biokinetics matched to the half-life of gallium-68. The scFv, J591c-scFv, was engineered with a C-terminal cysteine.
resultsJ591c-scFv was produced in HEK293T cells and purified by size-exclusion chromatography. A maleimide THP derivative (THP-mal) was coupled site-specifically to the C-terminal cysteine residue. The THP-mal-J591c-scFv conjugate was labelled with ammonium acetate-buffered gallium-68 from a
conclusionsThe bifunctional chelator THP-mal enabled simple, rapid, quantitative, one-step room temperature radiolabelling of a protein with gallium-68 at neutral pH without a need for post-labelling purification. The resultant gallium-68 complex shows high affinity for PSMA and favourable in vivo targeting properties in a xenograft model of PCa.
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