Glutamic acid–valine–citrulline linkers ensure stability and efficacy of antibody–drug conjugates in mice

The valine-citrulline dipeptide, which is used as a cleavable linker for antibody-drug conjugates, is instable in mouse plasma. Here, the authors developed a glutamic acid–valine–citrulline tripeptide sequence as a stable alternative that still is susceptible to cathepsin-mediated cleavage.

Bibliographic Details
Main Authors: Yasuaki Anami, Chisato M. Yamazaki, Wei Xiong, Xun Gui, Ningyan Zhang, Zhiqiang An, Kyoji Tsuchikama
Format: Article
Language:English
Published: Nature Publishing Group 2018-06-01
Series:Nature Communications
Online Access:https://doi.org/10.1038/s41467-018-04982-3