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

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 su...

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Veröffentlicht in:Organic letters 2020-11, Vol.22 (21), p.8419-8423
Hauptverfasser: Lee, TaeJin, Kim, Ju Hwan, Kwon, Se Jeong, Park, Sun Hee, Kim, Jinyoung, Kang, Hyo Jin, Chung, Sang J
Format: Artikel
Sprache:eng
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Zusammenfassung: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.
ISSN:1523-7060
1523-7052
DOI:10.1021/acs.orglett.0c03049