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

20 Citations (Scopus)

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
Publication statusPublished - 7 May 2020
Externally publishedYes

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