化学
连接器
结合
组合化学
同种类的
肽
内化
立体化学
序列(生物学)
有效载荷(计算)
小分子
抗癌药
配体(生物化学)
机制(生物学)
抗体-药物偶联物
拟肽
分子
均相催化
催化作用
寡肽
药物发现
抗原
纳米颗粒
生物化学
作者
JunSeok Son,J. W. Seo,S Park,Hojin Yeom,Nayoung Ko,Y. Lee,Jinyoung Kim,Ju Hwan Kim,S Park,Taedong Han,Sang J. Chung
出处
期刊:Organic Letters
[American Chemical Society]
日期:2025-12-31
卷期号:28 (2): 764-767
标识
DOI:10.1021/acs.orglett.5c04902
摘要
A traceless O-acyl hydroxamate Fc-binding peptide linker enables rapid, scavenger-free, and site-selective conjugation at Lys248 of human IgG1. The resulting homogeneous DAR2 antibody-drug conjugates (ADCs) retain antigen binding and internalization with payload-dependent stability and cytotoxicity. The linker's intrinsic leaving-group mechanism ensures clean FcBP release and broad payload compatibility. This robust, scalable traceless Lys248 conjugation chemistry underpins investigational new drug (IND)-approved and nonclinical ADC pipelines, offering a predictable platform for next-generation ADC design.
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