Nature Communications (Jun 2018)
Glutamic acid–valine–citrulline linkers ensure stability and efficacy of antibody–drug conjugates in mice
Abstract
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.