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Mar. Drugs 2017, 15(1), 18; doi:10.3390/md15010018

Marine Antibody–Drug Conjugates: Design Strategies and Research Progress

1
Department of Biochemistry and Molecular Biology, Second Military Medical University, Shanghai 200433, China
2
Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China
3
Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032, China
These authors contribute equally to this paper.
*
Authors to whom correspondence should be addressed.
Academic Editor: Peer B. Jacobson
Received: 26 October 2016 / Revised: 30 December 2016 / Accepted: 4 January 2017 / Published: 13 January 2017
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Abstract

Antibody–drug conjugates (ADCs), constructed with monoclonal antibodies (mAbs), linkers, and natural cytotoxins, are innovative drugs developed for oncotherapy. Owing to the distinctive advantages of both chemotherapy drugs and antibody drugs, ADCs have obtained enormous success during the past several years. The development of highly specific antibodies, novel marine toxins’ applications, and innovative linker technologies all accelerate the rapid R&D of ADCs. Meanwhile, some challenges remain to be solved for future ADCs. For instance, varieties of site-specific conjugation have been proposed for solving the inhomogeneity of DARs (Drug Antibody Ratios). In this review, the usages of various natural toxins, especially marine cytotoxins, and the development strategies for ADCs in the past decade are summarized. Representative ADCs with marine cytotoxins in the pipeline are introduced and characterized with their new features, while perspective comments for future ADCs are proposed. View Full-Text
Keywords: marine toxins; antibody–drug conjugates; monoclonal antibody; targeted therapy marine toxins; antibody–drug conjugates; monoclonal antibody; targeted therapy
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Wang, Y.-J.; Li, Y.-Y.; Liu, X.-Y.; Lu, X.-L.; Cao, X.; Jiao, B.-H. Marine Antibody–Drug Conjugates: Design Strategies and Research Progress. Mar. Drugs 2017, 15, 18.

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