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Experimental study demonstrates site-selective IgG1 modification at Lys248 using O-acyl hydroxamate affinity labels, highlighting a robust platform for precise antibody conjugation.
We report the design and synthesis of O -acyl hydroxamates (OAHs) affinity labels for selective modification of human IgG1 at Lys248 via proximity-driven acylation. Optimized compound 7g exhibits high water stability and >99% site-selective conversion at Lys248 on Trastuzumab using only 3 equiv. Peptide mapping and fluorescence labeling confirm its precision, establishing 7g as a robust platform for efficient and site-selective antibody conjugation.
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Seo et al. (2025) studied this question.
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