Development of a hydroxamamide-based bifunctional chelating agent to prepare technetium-99m-labeled bivalent ligand probes
نویسندگان
چکیده
Abstract Hydroxamamide (Ham) is a thiol-free chelating agent that forms technetium-99m ( 99m Tc)-complexes with metal-to-ligand ratio of 1:2 under moderate reaction conditions. Therefore, Ham-based agents will produce Tc-labeled compounds bivalent targeting scaffold. For their universal usage, we developed novel bifunctional agent, “Ham-Mal”, maleimide group can easily conjugate thiol group, for to preparing ligand probes. Ham-Mal was synthesized by four-step reaction, and then reacted cysteine or c(RGDfC) Ham-Cys Ham-RGD. These precursors were TcO 4 - 10 min room temperature obtain Tc-(Ham-Cys) 2 Tc -(Ham-RGD) . The cellular uptake level Tc-(Ham-RGD) U87MG (high Integrin ɑ v β 3 expression) cells significantly higher than PC3 (low at 60 after the incubation, suppressed pre-treatment 15 excess c(RGDfK) peptide. In in vivo study U87MG/PC3 dual xenografted BALB/c-nu mice, radioactivity tumor tissue 360 administration results suggest may have potential as
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ژورنال
عنوان ژورنال: Scientific Reports
سال: 2021
ISSN: ['2045-2322']
DOI: https://doi.org/10.1038/s41598-021-98235-x