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Photochemistry is a rich source of inspiration for developing alternative methods to functionalize proteins with drug molecules, fluorophores, and radioactive probes. Here, we report the synthesis and photochemical reactivity of a modified diethylenediamine pentaacetic acid chelate that was derivatized with a light-responsive aryl azide group (DTPA-PEG 3 -ArN 3 , compound 1 ). The corresponding nonradioactive and radioactive nat/68 Ga 3+ and nat/111 In 3+ complexes of DTPA-PEG 3 -ArN 3 were synthesized and their physical and photochemical properties were studied to evaluate the potential of employing this ligand system in the photochemical synthesis of radiolabeled antibodies. Photodegradation kinetics revealed that irradiation with ultraviolet light (365 nm) induced rapid photoactivation of compound 1 and the metal complexes nat/68 Ga- 1   -  and nat/111 In- 1   -  . Light-induced reactions were complete in &lt;100 s, with measured first-order rate constants of 0.078 ± 0.045 s -1 , 0.093 ± 0.009 s -1 , and 0.117 ± 0.054 s -1 ( n = 2, per species) for compound 1 , na Ga- 1   -  , and na In- 1   -  , respectively. Photochemically induced bioconjugation reactions between DTPA-PEG 3 -ArN 3 and the monoclonal antibody trastuzumab, as well as pre- and postconjugation 68 Ga- and 111 In-radiolabeling experiments, were performed using either a one-pot or two-step strategy. Both approaches yielded radiolabeled trastuzumab ([ 68 Ga]GaDTPA-azepin-trastuzumab) with average radiochemical conversions of 3.9 ± 1.0% ( n = 4, one-pot), and 10.0 ± 1.0% ( n = 3, two-step). One-pot radiolabeling reactions with [ 111 In]InCl 3 produced the corresponding [ 111 In]InDTPA-azepin-trastuzumab radiotracer in a similar radiochemical conversion of 5.4 ± 0.8% ( n = 3). Radiochemical conversions for the desired bimolecular coupling between the chelate and the protein were comparatively low. This observation is likely caused by the high photoinduced reactivity of the compounds and subsequent competition with background reactions. Nevertheless, access to DTPA-PEG 3 -ArN 3 increases the scope of photoradiochemical methods to include metal ions like In 3+ hat form complexes with higher coordination numbers.

Synthesis and Photochemical Studies on Gallium and Indium Complexes of DTPA-PEG3-ArN3 for Radiolabeling Antibodies

Synthesis and Photochemical Studies on Gallium and Indium Complexes of DTPA-PEG₃-ArN₃ for Radiolabeling Antibodies