Known for more than 130 years, hypervalent iodine reagents are still leading to the discovery of new synthetic transformations nowaday due to their unique reactivity. Nevertheless, their application to biomolecule labelling has just started to be investigated in the last 5 years. Our groups have used stable cyclic hypervalent iodine reagents - EthynylBenziodoXolones (EBXs) - for the alkynylation of cysteines in proteins. We also demonstrated that hypervalent iodine reagents can be directly installed into biomolecules. Herein, we report a new approach for target identification based on the surface modification of proteins using hypervalent iodine reagents. In contrast to our previous work aiming for labelling cysteine with high selectivity, the new method is modifying all amino acids in a nearly statistic manner, enabling sufficient surface coverage to identify binding positions and structural changes in proteins. The method is therefore expected to find broad application in chemical biology.

Surface modification of biomolecules with hypervalent iodine reagents for target identification

ACS Fall 2021

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