Photoconjugation of an Fc-Specific Peptide Enables Efficient DAR 2 Antibody–Drug Conjugate Formation,Organic Letters

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Photoconjugation of an Fc-Specific Peptide Enables Efficient DAR 2 Antibody–Drug Conjugate Formation
Organic Letters ( IF 4.9 ) Pub Date : 2020-10-19 , DOI: 10.1021/acs.orglett.0c03049
TaeJin Lee _{1,

2} , Ju Hwan Kim ₂ , Se Jeong Kwon _{1,

2} , Sun Hee Park _{1,

2} , Jinyoung Kim ₃ , Hyo Jin Kang ₂ , Sang J Chung _{1,

2}

Affiliation

Antibody–drug conjugates (ADCs) in current clinical usage have been constructed via the nonspecific conjugation of drugs to antibodies, rendering the manufacturing processes difficult. In this study, a high-affinity IgG Fc-binding peptide equipped with a photoreactive amino acid was developed and successfully conjugated to Glu-382 of trastuzumab in a site-specific manner. The resulting conjugate was employed to generate a DAR 2 ADC product using click chemistry.

中文翻译：

Fc 特异性肽的光偶联可实现高效的 DAR 2 抗体-药物偶联物形成

目前临床使用的抗体-药物偶联物 (ADC) 是通过药物与抗体的非特异性偶联来构建的，这使得制造过程变得困难。在这项研究中，开发了一种配备光反应性氨基酸的高亲和力 IgG Fc 结合肽，并以位点特异性方式成功地与曲妥珠单抗的 Glu-382 偶联。所得偶联物用于使用点击化学生成 DAR 2 ADC 产物。

更新日期：2020-11-06

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