DNA-encoded library technology (ELT) is a powerful tool for target validation and hit identification in early stage drug discovery. The attached DNA tagging limits the chemistry that can be applied to the technology. Enzymatic catalysis is a highly attractive alternative to classic chemical and chemocatalytic synthesis because it enables organic synthesis in aqueous environments with high stereoselectivity. In this presentation we will report threonine aldolase-catalyzed on-DNA aldol reaction to form β-hydroxy-α-amino acids with high yield and good stereoselectivity. The broad aldehyde scope and three functional groups in the product make it a valuble reaction to add to the DNA-encoded library synthesis toolbox.

Application of enzymes to on-DNA reactions

ACS Spring Meeting 2021

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