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Molecules 2017, 22(8), 1281;

Tubulin Inhibitor-Based Antibody-Drug Conjugates for Cancer Therapy

Department of Pharmaceutical Sciences, University of Tennessee Health Science Center, 881 Madison Avenue, Room 561, Memphis, TN 38163, USA
These authors contributed equally to this work.
Author to whom correspondence should be addressed.
Received: 12 July 2017 / Accepted: 29 July 2017 / Published: 1 August 2017
(This article belongs to the Special Issue Tubulin Inhibitors)
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Antibody-drug conjugates (ADCs) are a class of highly potent biopharmaceutical drugs generated by conjugating cytotoxic drugs with specific monoclonal antibodies through appropriate linkers. Specific antibodies used to guide potent warheads to tumor tissues can effectively reduce undesired side effects of the cytotoxic drugs. An in-depth understanding of antibodies, linkers, conjugation strategies, cytotoxic drugs, and their molecular targets has led to the successful development of several approved ADCs. These ADCs are powerful therapeutics for cancer treatment, enabling wider therapeutic windows, improved pharmacokinetic/pharmacodynamic properties, and enhanced efficacy. Since tubulin inhibitors are one of the most successful cytotoxic drugs in the ADC armamentarium, this review focuses on the progress in tubulin inhibitor-based ADCs, as well as lessons learned from the unsuccessful ADCs containing tubulin inhibitors. This review should be helpful to facilitate future development of new generations of tubulin inhibitor-based ADCs for cancer therapy. View Full-Text
Keywords: antibody-drug conjugates; cytotoxic payloads; linker; monoclonal antibody; site-specific conjugation; tubulin inhibitors antibody-drug conjugates; cytotoxic payloads; linker; monoclonal antibody; site-specific conjugation; tubulin inhibitors

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Chen, H.; Lin, Z.; Arnst, K.E.; Miller, D.D.; Li, W. Tubulin Inhibitor-Based Antibody-Drug Conjugates for Cancer Therapy. Molecules 2017, 22, 1281.

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