Three-Component Protein Modification Using Mercaptobenzaldehyde Derivatives

• DOI: 10.1021/acs.orglett.9b01294
• Publication Date: 2019-05-06T19:17:37Z
• Authors: Yuanwei Dai; Jiaping Weng; Justin George; Huan Chen; Qishan Lin; Jun Wang; Maksim Royzen; Qiang Zhang
• Keywords: Bioconjugation; Linker; Component (thermodynamics); Biocompatible material; Payload (computing)

A chemoselective primary amine modification strategy that enables the three-component, one-pot bioconjugation is described. The specifically designed, mercaptobenzaldehyde-based bifunctional linker achieves highly selective and robust labeling under biocompatible conditions. This demonstrates wide functional group tolerance simple to prepare, which allowed facile payload incorporation. Finally, our studies have shown introduction of does not impair function modified protein such as insulin.