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

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Abstract

An anti-EGFR nanobody was labeled at the C-terminus with a lysosome-sorting NPGY (Asn-Pro-Gly-Tyr) motif via sortase-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.

Graphical abstract: Protein labeling approach to improve lysosomal targeting and efficacy of antibody–drug conjugates

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Supplementary files

Article information


Submitted
06 Feb 2020
Accepted
21 Feb 2020
First published
22 Feb 2020

Org. Biomol. Chem., 2020, Advance Article
Article type
Communication

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

Y. Han, Y. Da, M. Yu, Y. Cheng, X. Wang, J. Xiong, G. Guo, Y. Li, X. Jiang and X. Cai, Org. Biomol. Chem., 2020, Advance Article , DOI: 10.1039/D0OB00265H

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