A strategic Ser/Cys exchange in the catalytic triad unlocks an acyltransferase-mediated synthesis of thioesters and tertiary amides

作者: Martina L. Contente , David Roura Padrosa , Francesco Molinari , Francesca Paradisi

DOI: 10.1038/S41929-020-00539-0

关键词: Catalytic triadBiocatalysisCofactorThioesterAcyltransferaseCysteineEnzyme catalysisAmideCombinatorial chemistry

摘要: Expanding the toolbox of enzymatic reactions accessible to organic chemists is one of the major goals in biocatalysis. Here we describe the development of an acyltransferase variant from Mycobacterium smegmatis in which a strategic Ser/Cys exchange in the catalytic triad dramatically expanded its synthetic capability to yield a biocatalyst able to efficiently catalyse the formation of thioesters and tertiary amides in water. Preparative scale (250 mM) biotransformations were performed starting from different thiols and secondary amines with …

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