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Cited by 786

The DOI matches its Crossref record; 61 of the 61 references it cites were found in a registry or an index.

Antibody-drug conjugates: recent advances in conjugation and linker chemistries

Open access
Tsuchikama, Kyoji, An, Zhiqiang·2018·Protein & Cell
DOI 10.1007/s13238-016-0323-0
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Abstract

The antibody-drug conjugate (ADC), a humanized or human monoclonal antibody conjugated with highly cytotoxic small molecules (payloads) through chemical linkers, is a novel therapeutic format and has great potential to make a paradigm shift in cancer chemotherapy. This new antibody-based molecular platform enables selective delivery of a potent cytotoxic payload to target cancer cells, resulting in improved efficacy, reduced systemic toxicity, and preferable pharmacokinetics (PK)/pharmacodynamics (PD) and biodistribution compared to traditional chemotherapy. Boosted by the successes of FDA-approved Adcetris® and Kadcyla®, this drug class has been rapidly growing along with about 60 ADCs currently in clinical trials. In this article, we briefly review molecular aspects of each component (the antibody, payload, and linker) of ADCs, and then mainly discuss traditional and new technologies of the conjugation and linker chemistries for successful construction of clinically effective ADCs. Current efforts in the conjugation and linker chemistries will provide greater insights into molecular design and strategies for clinically effective ADCs from medicinal chemistry and pharmacology standpoints. The development of site-specific conjugation methodologies for constructing homogeneous ADCs is an especially promising path to improving ADC design, which will open the way for novel cancer therapeutics.

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Metadata

Authors
Tsuchikama, K., & An, Z.
Venue
Protein & Cell
Publisher
Oxford University Press (OUP)
Published
2016-10-14
Volume
9
Issue
1
Pages
33-46
ISSN
  • 1674-800X (ISSN-L)
  • 1674-8018
DOI
10.1007/s13238-016-0323-0
OpenAlex
W2531611585
Cited by
786
References
61
FWCI
32.33
Type
journal article
Language
en
Open access
gold

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CoChat. (2026). Citation check: Antibody-drug conjugates: recent advances in conjugation and linker chemistries. https://app.cochat.ai/papers/10.1007/s13238-016-0323-0
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Tsuchikama, K., & An, Z. (2018). Antibody-drug conjugates: recent advances in conjugation and linker chemistries. Protein & Cell. https://doi.org/10.1007/s13238-016-0323-0

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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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