Document Type

Article

Department/Program

Chemistry

Journal Title

BIOORGANIC CHEMISTRY

Pub Date

2-2-2018

Volume

76

Abstract

The efficient preparation of protein bioconjugates represents a route to novel materials, diagnostics, and therapeutics. We previously reported a novel bioorthogonal Glaser-Hay reaction for the preparation of covalent linkages between proteins and a reaction partner; however, deleterious protein degradation was observed under extended reaction conditions. Herein, we describe the systematic optimization of the reaction to increase coupling efficiency and decrease protein degradation. Two optimized conditions were identified varying either the pH of the reaction or the bidentate ligand employed, allowing for more rapid conjugations and/or less protein oxidation. (C) 2017 Elsevier Inc. All rights reserved.

DOI

10.1016/j.bioorg.2017.11.020

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