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Protein labeling approach to improve lysosomal targeting and efficacy of antibody-drug conjugates

  • Ying Han
  • , Yifan Da
  • , Mingjia Yu
  • , Yaping Cheng
  • , Xin Wang
  • , Jiale Xiong
  • , Guoying Guo
  • , Yan Li
  • , Xianxing Jiang
  • , Xiaoqing Cai*
  • *Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

Abstract

An anti-EGFR nanobody was labeled at the C-terminus with a lysosome-sorting NPGY (Asn-Pro-Gly-Tyr) motifviasortase-mediated ligation to enhance the engagement of the clathrin-mediated endocytosis. The synergistic effects of NPGY motif and nona-arginine peptide were found to induce robust internalization and lysosomal trafficking, which in turn improved anti-tumor activity of an antibody-drug conjugate.

Original languageEnglish
Pages (from-to)3229-3233
Number of pages5
JournalOrganic and Biomolecular Chemistry
Volume18
Issue number17
DOIs
StatePublished - 7 May 2020
Externally publishedYes

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