N-terminal alpha-amino group modification of antibodies using a site-selective click chemistry method

	N-terminal alpha-amino group modification of antibodies using a site-selective click chemistry method
	Dimitrov, Dimiter S.; Li, De-zhi; Han, Bing-nan; Wei, Rui; Yao, Gui-Yang; Chen, Zhizhen; Liu, Jie; Poon, Terence C. W.; Su, Wu; Zhu, Zhongyu
刊名	MABS
	2018
文献子类	期刊论文
英文摘要	Site-specific conjugation of small molecules to antibody molecules is a promising strategy for generation of antibody-drug conjugates. In this report, we describe the successful synthesis of a novel bifunctional molecule, 6-(azidomethyl)-2-pyridinecarboxyaldehyde (6-AM-2-PCA), which was used for conjugation of small molecules to peptides and antibodies. We demonstrated that 6-AM-2-PCA selectively reacted with N-terminal amino groups of peptides and antibodies. In addition, the azide group of 6-AM-2-PCA enabled copper-free click chemistry coupling with dibenzocyclooctyne-containing reagents. Bifunctional 6-AM-2-PCA mediated site-specific conjugation without requiring genetic engineering of peptides or antibodies. A key advantage of 6-AM-2-PCA as a conjugation reagent is its ability to modify proteins in a single step under physiological conditions that are sufficiently moderate to retain protein function. Therefore, this new click chemistry-based method could be a useful complement to other conjugation methods.
URL标识	查看原文
语种	英语
内容类型	期刊论文
源URL	[http://ir.siat.ac.cn:8080/handle/172644/14601]
专题	深圳先进技术研究院_医药所
推荐引用方式 GB/T 7714	Dimitrov, Dimiter S.,Li, De-zhi,Han, Bing-nan,et al. N-terminal alpha-amino group modification of antibodies using a site-selective click chemistry method[J]. MABS,2018.
APA	Dimitrov, Dimiter S..,Li, De-zhi.,Han, Bing-nan.,Wei, Rui.,Yao, Gui-Yang.,...&Zhao, Qi.(2018).N-terminal alpha-amino group modification of antibodies using a site-selective click chemistry method.MABS.
MLA	Dimitrov, Dimiter S.,et al."N-terminal alpha-amino group modification of antibodies using a site-selective click chemistry method".MABS (2018).