2024
DOI: 10.1021/acs.jmedchem.4c02178
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Positron Emission Tomography Imaging of Cathepsin B in Tumors with Activable Small Molecule Tracers

Huirong Li,
Yuelin Li,
Ke Li
et al.

Abstract: Cathepsin B (CTB) is overexpressed in several types of tumors, and precise evaluation of the CTB activity can offer a promising method for the early diagnosis of tumors. In this study, two CTBactivated positron emission tomography (PET) tracers, [ 68 Ga]NOTA-SFCVM and [ 68 Ga]NOTA-SFCVHEM, were developed for sensitive and specific detection of CTB. Both tracers undergo a click condensation between 2-cyano-6-aminobenzothiazole (CBT) and cysteine (Cys) to form a cyclization product, thereby enhancing and prolong… Show more

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