Efficient Radiolabeling of Proteins and Antibodies via Maleamate-Cysteine Bioconjugation

ACS Med Chem Lett. 2024 Apr 10;15(5):691-695. doi: 10.1021/acsmedchemlett.4c00092. eCollection 2024 May 9.

Abstract

The study introduces a novel maleamate-based prosthetic group specifically designed for efficient, site-specific radioiodination of biomolecules that contain or are modified with cysteine residues. This strategy is a compelling alternative to the conventional maleimide-based approach, demonstrating outstanding attributes such as high radiochemical yield, rapid reaction kinetics, applicability in aqueous media at neutral pH, and exceptional stability under a competitive environment.