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Int. J. Mol. Sci. 2016, 17(2), 194; doi:10.3390/ijms17020194

Methods to Design and Synthesize Antibody-Drug Conjugates (ADCs)

1,* and 1,*
Institute for Advancing Translational Medicine in Bone & Joint Diseases, School of Chinese Medicine, Hong Kong Baptist University, Hong Kong, China
Faculty of Materials Science and Chemical Engineering, the State Key Laboratory Base of Novel Functional Materials and Preparation Science, Ningbo University, Ningbo 315211, Zhejiang, China
These authors contributed equally to this work.
Authors to whom correspondence should be addressed.
Academic Editor: Már Másson
Received: 11 January 2016 / Revised: 28 January 2016 / Accepted: 28 January 2016 / Published: 2 February 2016
(This article belongs to the Section Biochemistry, Molecular and Cellular Biology)
View Full-Text   |   Download PDF [4709 KB, uploaded 2 February 2016]   |  


Antibody-drug conjugates (ADCs) have become a promising targeted therapy strategy that combines the specificity, favorable pharmacokinetics and biodistributions of antibodies with the destructive potential of highly potent drugs. One of the biggest challenges in the development of ADCs is the application of suitable linkers for conjugating drugs to antibodies. Recently, the design and synthesis of linkers are making great progress. In this review, we present the methods that are currently used to synthesize antibody-drug conjugates by using thiols, amines, alcohols, aldehydes and azides. View Full-Text
Keywords: antibody-drug conjugates (ADCs); targeted therapy; monoclonal antibodies (mAbs); drugs; linkers antibody-drug conjugates (ADCs); targeted therapy; monoclonal antibodies (mAbs); drugs; linkers

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Yao, H.; Jiang, F.; Lu, A.; Zhang, G. Methods to Design and Synthesize Antibody-Drug Conjugates (ADCs). Int. J. Mol. Sci. 2016, 17, 194.

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