Nature Communications (Jun 2018)

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

  • Yasuaki Anami,
  • Chisato M. Yamazaki,
  • Wei Xiong,
  • Xun Gui,
  • Ningyan Zhang,
  • Zhiqiang An,
  • Kyoji Tsuchikama

DOI
https://doi.org/10.1038/s41467-018-04982-3
Journal volume & issue
Vol. 9, no. 1
pp. 1 – 9

Abstract

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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.