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 |
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Hauptverfasser: | , , , , , , |
Format: | Artikel |
Sprache: | eng |
Online-Zugang: | Volltext |
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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. |
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ISSN: | 1523-7060 1523-7052 |
DOI: | 10.1021/acs.orglett.0c03049 |