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The Capital Region of Denmark - a part of Copenhagen University Hospital
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Affinity-Guided Conjugation to Antibodies for Use in Positron Emission Tomography

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The radionuclide copper-64 is widely used in combination with biomolecules, such as antibodies, for positron emission tomography (PET). Copper-64 is ideal for the imaging of biomolecules with long circulation times due to its relatively long half-life, and when conjugated to an antibody, specific cells can be targeted in vivo. Here, we have prepared a trastuzumab-chelator conjugate by using affinity-guided conjugation, in which an azide was attached to the antibody prior to a strain promoted azide-alkyne cycloaddition reaction with DBCO-PEG4-NOTA. The conjugate was benchmarked against a standard nonspecific labeled trastuzumab-NOTA conjugate. The conjugates were tested for incorporation of copper-64, stability in buffer and plasma, and tumor targeting in vivo using PET imaging of mice with xenograft tumors expressing HER2. Both conjugates showed good incorporation of copper-64 and a high stability with less than 10% degradation after 36 h. Furthermore, both conjugates showed accumulation at the tumor site with mean uptake of 7.2 ± 2.4%ID/g and 5.2 ± 1.3%ID/g after 40 h for the affinity-guided labeled trastuzumab and the nonspecific labeled trastuzumab, respectively.

Original languageEnglish
JournalBioconjugate Chemistry
Volume30
Issue number3
Pages (from-to)881-887
Number of pages7
ISSN1043-1802
DOIs
Publication statusPublished - 20 Mar 2019

    Research areas

  • Animals, Antibodies/administration & dosage, Humans, Mice, Positron-Emission Tomography/methods, Trastuzumab/administration & dosage

ID: 59322615