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N-terminal α-amino group modification of antibodies using a site-selective click chemistry method
Li D.-Z.6; Han B.-N.1; Wei R.2; Yao G.-Y.5; Chen Z.2; Liu J.2; Poon T.C.W.2; Su W.5; Zhu Z.3; Dimitrov D.S.4; Zhao Q.2
2018-07-04
Source PublicationmAbs
ISSN19420870 19420862
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
URLView the original
Indexed BySCI
Language英语
WOS Research AreaResearch & Experimental Medicine
WOS SubjectMedicine, Research & Experimental
WOS IDWOS:000437354300002
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Cited Times [WOS]:7   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionFaculty of Health Sciences
Affiliation1.Zhejiang Sci-Tech University
2.Universidade de Macau
3.National Cancer Institute
4.University of Pittsburgh School of Medicine
5.Chinese Academy of Sciences
6.Peking University
Recommended Citation
GB/T 7714
Li D.-Z.,Han B.-N.,Wei R.,et al. N-terminal α-amino group modification of antibodies using a site-selective click chemistry method[J]. mAbs,2018,10(5):712-719.
APA Li D.-Z..,Han B.-N..,Wei R..,Yao G.-Y..,Chen Z..,...&Zhao Q..(2018).N-terminal α-amino group modification of antibodies using a site-selective click chemistry method.mAbs,10(5),712-719.
MLA Li D.-Z.,et al."N-terminal α-amino group modification of antibodies using a site-selective click chemistry method".mAbs 10.5(2018):712-719.
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