Issue 1, 2017

Decoupling stability and release in disulfide bonds with antibody-small molecule conjugates

Abstract

Disulfide bonds provide a bioactivatable connection with applications in imaging and therapy. The circulation stability and intracellular release of disulfides are problematically coupled in that increasing stability causes a corresponding decrease in cleavage and payload release. However, an antibody offers the potential for a reversible stabilization. We examined this by attaching a small molecule directly to engineered cysteines in an antibody. At certain sites this unhindered disulfide was stable in circulation yet cellular internalization and antibody catabolism generated a disulfide catabolite that was rapidly reduced. We demonstrated that this stable connection and facile release is applicable to a variety of payloads. The ability to reversibly stabilize a labile functional group with an antibody may offer a way to improve targeted probes and therapeutics.

Graphical abstract: Decoupling stability and release in disulfide bonds with antibody-small molecule conjugates

Supplementary files

Article information

Article type
Edge Article
Submitted
26 Apr 2016
Accepted
10 Aug 2016
First published
22 Aug 2016
This article is Open Access

All publication charges for this article have been paid for by the Royal Society of Chemistry
Creative Commons BY license

Chem. Sci., 2017,8, 366-370

Decoupling stability and release in disulfide bonds with antibody-small molecule conjugates

T. H. Pillow, J. D. Sadowsky, D. Zhang, S. Yu, G. Del Rosario, K. Xu, J. He, S. Bhakta, R. Ohri, K. R. Kozak, E. Ha, J. R. Junutula and J. A. Flygare, Chem. Sci., 2017, 8, 366 DOI: 10.1039/C6SC01831A

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements