Catalyst-free site-selective cross-aldol bioconjugations

16 June 2022, Version 1
This content is a preprint and has not undergone peer review at the time of posting.


The bioconjugation of proteins to small molecules serves as an invaluable tool for probing biological mechanisms and creating biomaterials. The most powerful bioconjugation stratagems are those which have rapid kinetics, are site-selective, can be conducted in aqueous solvent under mild conditions and do not require the use of additional potentially toxic catalysts. Herein we present spontaneous coupling via aldol ligation of proteins (SCALP) a catalyst-free “green” site-selective protein ligation between α-oxo aldehyde functionalised proteins and enolisable aldehyde probes at neutral pH, and demonstrate the utility of this system in the targeting of prostate cancer cells with functionalised nanobodies.



Supplementary materials

Supplementary information_Catalyst-free site-selective cross-aldol bioconjugations
The Supporting Information includes all data accompanying this paper including details of the preparation of JVZ007, the synthesis and characterisation of organic compounds/probes and the method used for SDS-PAGE and western blot analyses.


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