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N-terminal alpha-amino group modification of antibodies using a site-selective click chemistry method
De-zhi Li1; Bing-nan Han2; Rui Wei3; Gui-yang Yao4; Zhizhen Chen3; Jie Liu3; Terence C.W. Poon3; Wu Su4; Zhongyu Zhu5; Dimiter S. Dimitrov6; Qi Zhao3
2018
Source PublicationMABS
ISSN1942-0862
Volume10Issue:5Pages:712-719
Abstract

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.

KeywordAntibody Antibody Engineering Antibody-drug Conjugate Click Chemistry Site-specific Modification
DOI10.1080/19420862.2018.1463122
Indexed BySCIE
Language英语
WOS Research AreaResearch & Experimental Medicine
WOS SubjectMedicine, Research & Experimental
WOS IDWOS:000437354300002
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Cited Times [WOS]:10   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionFaculty of Health Sciences
Corresponding AuthorQi Zhao
Affiliation1.Peking University Shenzhen Hospital, Shenzhen PKU-HKUST Medical Center, Guangdong, China
2.Department of Development Technology of Marine Resources, School of Life Science, Zhejiang Sci-Tech University, Zhejiang, China
3.Faculty of Health Sciences, University of Macau, Macau, China
4.Shenzhen Institutes of Advanced Technology, Chinese Academy of Sciences, Guangdong, China
5.Cancer and Inflammation Program, Center for Cancer Research, National Cancer Institute, Frederick, NIH, USA
6.Department of Medicine, Center for Antibody Therapeutics, University of Pittsburgh Medical School, Pennsylvania, USA
Corresponding Author AffilicationFaculty of Health Sciences
Recommended Citation
GB/T 7714
De-zhi Li,Bing-nan Han,Rui Wei,et al. N-terminal alpha-amino group modification of antibodies using a site-selective click chemistry method[J]. MABS,2018,10(5):712-719.
APA De-zhi Li.,Bing-nan Han.,Rui Wei.,Gui-yang Yao.,Zhizhen Chen.,...&Qi Zhao.(2018).N-terminal alpha-amino group modification of antibodies using a site-selective click chemistry method.MABS,10(5),712-719.
MLA De-zhi Li,et al."N-terminal alpha-amino group modification of antibodies using a site-selective click chemistry method".MABS 10.5(2018):712-719.
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