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Balancing Reactivity and Specificity: Fc-Binding O-Acyl Hydroxamate Reagents for Site-Selective Antibody Labeling at Lys248
- Seo, Jin Woo;
- Park, Sun Hee;
- Kim, Jinyoung;
- Lee, Taejin;
- Park, Seong-Hyun;
- ... Chung, Sang J.;
- 외 2명
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2초록
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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CONJUGATION; ENABLES
- 제목
- Balancing Reactivity and Specificity: Fc-Binding O-Acyl Hydroxamate Reagents for Site-Selective Antibody Labeling at Lys248
- 저자
- Seo, Jin Woo; Park, Sun Hee; Kim, Jinyoung; Lee, Taejin; Park, Seong-Hyun; Kim, Ju Hwan; Han, Taedong; Chung, Sang J.
- 발행일
- 2025-05
- 유형
- Letter
- 저널명
- Organic Letters
- 권
- 27
- 호
- 22
- 페이지
- 5665 ~ 5668