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Cited by 285

The DOI matches its Crossref record; 95 of the 95 references it cites were found in a registry or an index.

Linkers Having a Crucial Role in Antibody–Drug Conjugates

Open access
Lu, Jun, Jiang, Feng, Lu, Aiping, Zhang, Ge·2016·International Journal of Molecular Sciences

Abstract

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.

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Metadata

Authors
Lu, J., Jiang, F., Lu, A., & Zhang, G.
Venue
International Journal of Molecular Sciences
Publisher
MDPI AG
Published
2016-04-14
Volume
17
Issue
4
Pages
561
ISSN
1422-0067 (ISSN-L)
OpenAlex
W2337546548
Cited by
285
References
95
FWCI
16.56
Type
journal article
Language
en
Open access
gold

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CoChat. (2026). Citation check: Linkers Having a Crucial Role in Antibody–Drug Conjugates. https://app.cochat.ai/papers/10.3390/ijms17040561
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Lu, J., Jiang, F., Lu, A., & Zhang, G. (2016). Linkers Having a Crucial Role in Antibody–Drug Conjugates. International Journal of Molecular Sciences. https://doi.org/10.3390/ijms17040561

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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).

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