Abstract
The modification of biomolecules is significant to chemical biology. One of the challenges is improving the trans-membrane transport, and recently vitamin B[Formula: see text] has emerged as a biocompatible transporter that can facilitate the uptake. This study investigates the formation of adducts between vitamin B[Formula: see text] thiolate and 5HP2O linkers (5-hydroxy-1,5-dihydro-2[Formula: see text]-pyrrol-2-ones) as a novel approach to converting native B[Formula: see text] into versatile bioconjugation-ready intermediates. We synthesized two model 5HP2O linkers and optimized the reaction with the readily available and bench-stable isothiouronium salt of vitamin B[Formula: see text] that generates reactive thiolate in situ. The optimal conditions included using a 1:1 mixture of H2O/EtOH or H2O/DMSO as solvents, excess of 5HP2O, and methylamine, at the concentration of 3.5 mM. This work enriches the bioconjugation toolkit and offers new insights into the development of vitamin B[Formula: see text]-containing therapeutics.
Published Version
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