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

Org Lett. 2020 Nov 6;22(21):8419-8423. doi: 10.1021/acs.orglett.0c03049. Epub 2020 Oct 19.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antibody Specificity*
  • Click Chemistry
  • Immunoconjugates / chemistry*
  • Immunoglobulin Fc Fragments / immunology*
  • Peptides / chemistry*
  • Trastuzumab / chemistry

Substances

  • Immunoconjugates
  • Immunoglobulin Fc Fragments
  • Peptides
  • Trastuzumab