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Bioconjugation

How to pick a single amine?

Single-step site-specific labeling of native proteins is one of the holy grails in the chemical biology field. 2-Pyridinecarboxyaldehyde derivatives are shown to react selectively at the N terminus of proteins to form stable conjugates, irrespective of the nature of the N-terminal amino acid, enabling the straightforward introduction of useful functional groups into a wide array of proteins.

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Figure 1: Basis of the selectivity for the N terminus of proteins by participation of the adjacent amide substituent.

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Correspondence to Floris P J T Rutjes.

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Rutjes, F. How to pick a single amine?. Nat Chem Biol 11, 306–307 (2015). https://doi.org/10.1038/nchembio.1791

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