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Decoupling stability and release in disulfide bonds with antibody-small molecule conjugates†
Thomas H. Pillow,Jack D. Sadowsky,Donglu Zhang,Shang-Fan Yu,Geoffrey Del Rosario,Keyang Xu,Jintang He,Sunil Bhakta,Rachana Ohri,Katherine R. Kozak,Edward Ha,Jagath R. Junutula,John A. Flygare
Chemical Science Pub Date : 08/22/2016 00:00:00 , DOI:10.1039/C6SC01831A
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
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