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Methods Enzymol. 2012;502:123-38. doi: 10.1016/B978-0-12-416039-2.00006-9.

Conjugation of anticancer drugs through endogenous monoclonal antibody cysteine residues.

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  • 1Seattle Genetics, Bothell, Washington, USA.


Many methods have been described for the conjugation of drugs to monoclonal antibodies. The presence of a discrete number of readily reducible disulfides in the common IgG subtypes presents a convenient opportunity for conjugation to cysteine residues with thiol-reactive drug-linkers. Such conjugates can be prepared by a straightforward two-step reaction scheme involving the reduction of the antibody disulfides to the desired number of average thiols per antibody, followed by addition of the drug-linker, ideally with a maleimido functionality for rapid, selective reaction. In a discovery setting, this basic method can be scaled down to produce microgram quantities of conjugate for early screening, and in a manufacturing setting can be scaled up to produce grams or kilograms of conjugate for clinical trials and commercialization. The resulting conjugates are readily characterized using common HPLC methods.

Copyright © 2012 Elsevier Inc. All rights reserved.

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