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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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
Materias:	Science Q
Acceso en línea:	https://doaj.org/article/8436b2df5ee445a5b2278b4b789128d3
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id	oai:doaj.org-article:8436b2df5ee445a5b2278b4b789128d3
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spelling	oai:doaj.org-article:8436b2df5ee445a5b2278b4b789128d32021-12-02T17:32:30ZGlutamic acid–valine–citrulline linkers ensure stability and efficacy of antibody–drug conjugates in mice10.1038/s41467-018-04982-32041-1723https://doaj.org/article/8436b2df5ee445a5b2278b4b789128d32018-06-01T00:00:00Zhttps://doi.org/10.1038/s41467-018-04982-3https://doaj.org/toc/2041-1723The 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.Yasuaki AnamiChisato M. YamazakiWei XiongXun GuiNingyan ZhangZhiqiang AnKyoji TsuchikamaNature PortfolioarticleScienceQENNature Communications, Vol 9, Iss 1, Pp 1-9 (2018)
institution	DOAJ
collection	DOAJ
language	EN
topic	Science Q
spellingShingle	Science Q Yasuaki Anami Chisato M. Yamazaki Wei Xiong Xun Gui Ningyan Zhang Zhiqiang An Kyoji Tsuchikama Glutamic acid–valine–citrulline linkers ensure stability and efficacy of antibody–drug conjugates in mice
description	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.
format	article
author	Yasuaki Anami Chisato M. Yamazaki Wei Xiong Xun Gui Ningyan Zhang Zhiqiang An Kyoji Tsuchikama
author_facet	Yasuaki Anami Chisato M. Yamazaki Wei Xiong Xun Gui Ningyan Zhang Zhiqiang An Kyoji Tsuchikama
author_sort	Yasuaki Anami
title	Glutamic acid–valine–citrulline linkers ensure stability and efficacy of antibody–drug conjugates in mice
title_short	Glutamic acid–valine–citrulline linkers ensure stability and efficacy of antibody–drug conjugates in mice
title_full	Glutamic acid–valine–citrulline linkers ensure stability and efficacy of antibody–drug conjugates in mice
title_fullStr	Glutamic acid–valine–citrulline linkers ensure stability and efficacy of antibody–drug conjugates in mice
title_full_unstemmed	Glutamic acid–valine–citrulline linkers ensure stability and efficacy of antibody–drug conjugates in mice
title_sort	glutamic acid–valine–citrulline linkers ensure stability and efficacy of antibody–drug conjugates in mice
publisher	Nature Portfolio
publishDate	2018
url	https://doaj.org/article/8436b2df5ee445a5b2278b4b789128d3
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Glutamic acid–valine–citrulline linkers ensure stability and efficacy of antibody–drug conjugates in mice

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