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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2

초록

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.

키워드

CONJUGATIONENABLES
제목
Balancing Reactivity and Specificity: Fc-Binding O-Acyl Hydroxamate Reagents for Site-Selective Antibody Labeling at Lys248
저자
Seo, Jin WooPark, Sun HeeKim, JinyoungLee, TaejinPark, Seong-HyunKim, Ju HwanHan, TaedongChung, Sang J.
DOI
10.1021/acs.orglett.5c01424
발행일
2025-05
유형
Letter
저널명
Organic Letters
27
22
페이지
5665 ~ 5668