ArticleMolecular imaging and biology2026
Macrocycle Chelator Conjugation on the C3 Hydroxyl Group of 17β-Estradiol reduces Estrogen Receptor Binding.
Article in Molecular imaging and biology, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
purposeTumor heterogeneity in breast cancer complicates accurate molecular characterization when using standard-of-care imaging modalities. In this study, gallium-68 labeled estradiol-derivatives were synthesized and evaluated as candidate tracers to be used for multiplexed PET imaging with the goal of improving the molecular characterization of breast cancer. PROCEDURES: 17β-estradiol was conjugated to DOTA and NODAGA macrocycles and radiolabeled with gallium-68. The selectivity of the resulting radiotracers, [
resultsBoth radiotracers were obtained with high radiochemical purity. Neither [
conclusionTwo estradiol-derived radiotracers were successfully synthesized and tested, however neither showed selective binding towards ER in vitro or in vivo. The conjugation site of the cyclic macrocycle on 17β-estradiol is likely a key parameter to retain strong binding towards ER. These findings identify an important limitation for chelator-based ER tracer design.
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