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β-Galactosidase-guided self-assembled 68 Ga nanofibers probe for micro-PET tumor imaging.
Bioorganic & Medicinal Chemistry Letters 2024 April 5
β-galactosidase (β-gal) has high activity in various malignancies, which is suitable for targeted positron emission tomography (PET) imaging. Meanwhile, β-gal can successfully guide the formation of nanofibers, which enhances the intensity of imaging and extends the imaging time. Herein, we designed a β-galactosidase-guided self-assembled PET imaging probe [68 Ga]Nap-NOTA-1Gal. We envisage that β-gal could recognize and cleave the target site, bringing about self-assembling to form nanofibers, thereby enhancing the PET imaging effect. The targeting specificity of [68 Ga]Nap-NOTA-1Gal for detecting β-gal activity was examined using the control probe [68 Ga]Nap-NOTA-1. Micro-PET imaging showed that tumor regions of [68 Ga]Nap-NOTA-1Gal were visible after injection. And the tumor uptake of [68 Ga]Nap-NOTA-1Gal was higher than [68 Ga]Nap-NOTA-1 at all-time points. Our results demonstrated that the [68 Ga]Nap-NOTA-1Gal can be used for the purpose of a new promising PET probe for helping diagnose cancer with high levels of β-gal activity.
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