Heptadentate chelates for ⁸⁹Zr-radiolabelling of monoclonal antibodies.

ABSTRACT: Herein, we report the synthesis of three new bifunctional heptadentate metal ion binding chelates derived from desferrioxamine B (DFO) linked to a tripeptide unit that comprises of a glutamic acid and two glycine residues. The three DFO derivatives were also functionalised with a photoactivatable aryl azide unit for light-triggered labelling of proteins. The chelates were obtained in 3 synthetic steps in good overall yields by using solid phase peptide synthesis (SPPS). Density Functional Theory (DFT) calculations were used to estimate thermodynamic formation constants (log β) of the corresponding Zr⁴⁺ complexes. Quantitative zirconium-89 radiolabelling (>95%) was obtained in <5 min at room temperature, and the stability of the radioconjugates toward different competitors

SUBMITTER: Guillou A 

PROVIDER: S-EPMC9196204 | biostudies-literature | 2022 Jun

REPOSITORIES: biostudies-literature