Site-Selective Antibody–Drug Conjugation by a Proximity-Driven S to N Acyl Transfer Reaction on a Therapeutic Antibody

Immunoglobulin Gs (IgGs) contain many Lys and Cys residues, which results in an unwanted complex product mixture with conventional drug conjugation methods. We selectively acylated the ε-NH2 of K248 on trastuzumab using an IgG Fc-binding peptide (FcBP) equipped with a 5-norbornene-2-carboxylic acid...

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Veröffentlicht in:	Journal of medicinal chemistry 2022-04, Vol.65 (7), p.5751-5759
Hauptverfasser:	Lee, TaeJin, Kim, Ju Hwan, Kwon, Se Jeong, Seo, Jin Woo, Park, Sun Hee, Kim, Jinyoung, Jin, Jonghwa, Hong, Ji Hye, Kang, Hyo Jin, Sharma, Chiranjeev, Choi, Ji Hoon, Chung, Sang J
Format:	Artikel
Sprache:	eng
Schlagworte:	Immunoconjugates - chemistry Peptides Trastuzumab - chemistry
Online-Zugang:	Volltext
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