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Issue 1, 2013
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Spacer length shapes drug release and therapeutic efficacy of traceless disulfide-linked ADCs targeting the tumor neovasculature

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Abstract

We systematically investigated how the therapeutic efficacy of a traceless, vascular targeting antibody–drug conjugate (ADC) is affected by the length of a spacer introduced between the antibody's globular fold and the site of drug attachment. Homogeneous ADCs were prepared from the direct conjugation of engineered C-terminal cysteines with a potent thiol containing drug which was separated from the antibody surface by unstructured spacers of increasing length. We found that a smaller spacer length is reflected in enhanced stability and therapeutic efficacy of the conjugates in a syngeneic model of murine cancer.

Graphical abstract: Spacer length shapes drug release and therapeutic efficacy of traceless disulfide-linked ADCs targeting the tumor neovasculature

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Article information


Submitted
28 Jul 2012
Accepted
05 Oct 2012
First published
08 Oct 2012

Chem. Sci., 2013,4, 297-302
Article type
Edge Article

Spacer length shapes drug release and therapeutic efficacy of traceless disulfide-linked ADCs targeting the tumor neovasculature

M. Steiner, I. Hartmann, E. Perrino, G. Casi, S. Brighton, I. Jelesarov, G. J. L. Bernardes and D. Neri, Chem. Sci., 2013, 4, 297
DOI: 10.1039/C2SC21107F

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