Site-Selective Antibody Conjugation with Dibromopyrazines

Szepesi Kovács, Dénes and Ábrányi-Balogh, Péter and Keserű, György Miklós (2024) Site-Selective Antibody Conjugation with Dibromopyrazines. BIOCONJUGATE CHEMISTRY, 35 (9).

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Abstract

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.

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