Affinity-Guided Conjugation to Antibodies for Use in Positron Emission Tomography

Bioconjug Chem. 2019 Mar 20;30(3):881-887. doi: 10.1021/acs.bioconjchem.9b00013. Epub 2019 Mar 12.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

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

Substances

  • Antibodies
  • Trastuzumab