biostudies-literatureUnknown12(26)Rudd SEAustralian Cancer Research FoundationNational Health and Medical Research CouncilAustralian Research CouncilIdentification of tumors which over-express Epidermal Growth Factor Receptor (EGFR) is important in selecting patients for anti-EGFR therapies. Enzymatic bioconjugation was used to introduce positron-emitting radionuclides (⁸⁹Zr, ⁶⁴Cu) into an anti-EGFR antibody fragment for Positron Emission Tomography (PET) imaging the same day as injection. A monovalent antibody fragment with high affinity for EGFR was engineered to include a sequence that is recognized by the transpeptidase sortase A. Two different metal chelators, one for ⁸⁹Zr^IV and one for ⁶⁴Cu^II, were modified with a N-terminal glycine to enable them to act as substrates in sortase A mediated bioconjugation to the antibody fragment. Both fragments provided high-qualitChemical science9004-9016https://www.ebi.ac.uk/biostudies/studies/S-EPMC8261882biostudies-literatureEnzyme mediated incorporation of zirconium-89 or copper-64 into a fragment antibody for same day imaging of epidermal growth factor receptor.PMC8261882Pearce LACullinane CHicks RJRaicevic ARudd SEVan Zuylekom JKAdams TEDonnelly PSWilliams CCfalseEnzyme mediated incorporation of zirconium-89 or copper-64 into a fragment antibody for same day imaging of epidermal growth factor receptor.Identification of tumors which over-express Epidermal Growth Factor Receptor (EGFR) is important in selecting patients for anti-EGFR therapies. Enzymatic bioconjugation was used to introduce positron-emitting radionuclides (⁸⁹Zr, ⁶⁴Cu) into an anti-EGFR antibody fragment for Positron Emission Tomography (PET) imaging the same day as injection. A monovalent antibody fragment with high affinity for EGFR was engineered to include a sequence that is recognized by the transpeptidase sortase A. Two different metal chelators, one for ⁸⁹Zr^IV and one for ⁶⁴Cu^II, were modified with a N-terminal glycine to enable them to act as substrates in sortase A mediated bioconjugation to the antibody fragment. Both fragments provided high-qualit2021-01-01T00:00:00Z2021 Jul2026-06-02T12:30:06.608Z2022-02-10T20:31:44.061ZS-EPMC82618823427692810.1039/d1sc01422f