Photocatalytic acylation of lysine screened using a microfluidic-based chemical robotic system†

The application scope of various bioconjugation technologies has been expanded through the implementation of photoredox catalytic bioconjugation technology, establishing a novel biomolecular framework with exceptional residue selectivity. Herein, we report a facile acylation reaction utilizing a thioacid and a photoexcited riboflavin tetraacetate (RFTA) catalyst under visible light (450 nm). The optimal reaction conditions were obtained using a high-throughput microfluidic-based chemical robotic system and GPR model. We have successfully modified a range of proteins and antibodies and utilized the functional handle to attach diverse biological molecules, demonstrating the versatility and generality of our approach. In addition, this photoredox catalytic reaction was also successfully employed in peptide modification, protein labeling, and antibody conjugation.