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Site-Selective Antibody Conjugation with Dibromopyrazines

Bioconjugate Chemistry, ISSN: 1520-4812, Vol: 35, Issue: 9, Page: 1373-1379
2024
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Article Description

In recent years, antibody conjugates have evolved as state-of-the-art options for diagnostic and therapeutic applications. During site-selective antibody conjugation, incomplete rebridging of antibody chains limits the homogeneity of conjugates and calls for the development of new rebridging agents. Herein, we report a dibromopyrazine derivative optimized to reach highly homogeneous conjugates rapidly and with high conversion on rebridging of trastuzumab, even providing a feasible route for antibody modification in acidic conditions. Furthermore, coupling a fluorescent dye and a cytotoxic drug resulted in effective antibody conjugates with excellent serum stability and in vitro selectivity, demonstrating the utility of the dibromopyrazine rebridging agent to produce on-demand future antibody conjugates for diagnostic or therapeutic applications.

Bibliographic Details

Szepesi Kovács, Dénes; Pásztor, Bettina; Ábrányi-Balogh, Péter; Petri, László; Imre, Tímea; Simon, József; Tátrai, Enikő; Várady, György; Tóvári, József; Szijj, Peter A; Keserű, György M

American Chemical Society (ACS)

Biochemistry, Genetics and Molecular Biology; Chemical Engineering; Engineering; Pharmacology, Toxicology and Pharmaceutics; Chemistry

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