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Int. J. Mol. Sci. 2016, 17(4), 561;

Linkers Having a Crucial Role in Antibody–Drug Conjugates

1,2,* and 1,2,*
Institute for Advancing Translational Medicine in Bone & Joint Diseases, School of Chinese Medicine, Hong Kong Baptist University, Hong Kong, China
Institute of Integrated Bioinfomedicine & Translational Science, Hong Kong Baptist University Shenzhen Research Institute and Continuing Education, Shenzhen 518000, China
Institute of Precision Medicine and Innovative Drug Discovery, HKBU (Haimen) Institute of Science and Technology, Haimen 226100, China
These authors contributed equally to this work.
Authors to whom correspondence should be addressed.
Academic Editor: Wenbin Deng
Received: 21 February 2016 / Revised: 29 March 2016 / Accepted: 8 April 2016 / Published: 14 April 2016
(This article belongs to the Special Issue Translational Molecular Medicine & Molecular Drug Discovery)
Full-Text   |   PDF [3579 KB, uploaded 14 April 2016]   |  


Antibody–drug conjugates (ADCs) comprised of a desirable monoclonal antibody, an active cytotoxic drug and an appropriate linker are considered to be an innovative therapeutic approach for targeted treatment of various types of tumors and cancers, enhancing the therapeutic parameter of the cytotoxic drug and reducing the possibility of systemic cytotoxicity. An appropriate linker between the antibody and the cytotoxic drug provides a specific bridge, and thus helps the antibody to selectively deliver the cytotoxic drug to tumor cells and accurately releases the cytotoxic drug at tumor sites. In addition to conjugation, the linkers maintain ADCs’ stability during the preparation and storage stages of the ADCs and during the systemic circulation period. The design of linkers for ADCs is a challenge in terms of extracellular stability and intracellular release, and intracellular circumstances, such as the acid environment, the reducing environment and cathepsin, are considered as the catalysts to activate the triggers for initiating the cleavage of ADCs. This review discusses the linkers used in the clinical and marketing stages for ADCs and details the fracture modes of the linkers for the further development of ADCs. View Full-Text
Keywords: antibody–drug conjugates; cytotoxic drug; monoclonal antibody; linker; attachment site; tumor antibody–drug conjugates; cytotoxic drug; monoclonal antibody; linker; attachment site; tumor

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Lu, J.; Jiang, F.; Lu, A.; Zhang, G. Linkers Having a Crucial Role in Antibody–Drug Conjugates. Int. J. Mol. Sci. 2016, 17, 561.

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