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.

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Detalles Bibliográficos
Autores principales: Yasuaki Anami, Chisato M. Yamazaki, Wei Xiong, Xun Gui, Ningyan Zhang, Zhiqiang An, Kyoji Tsuchikama
Formato: article
Lenguaje:EN
Publicado: Nature Portfolio 2018
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Acceso en línea:https://doaj.org/article/8436b2df5ee445a5b2278b4b789128d3
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Sumario: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.