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Identification and Application of Threonine Aldolase for Synthesis of valuable α-amino, β-hydroxy-Building Blocks

Ligibel, Mathieu and Moore, Charles and Bruccoleri, Robert and Snajdrova, Radka (2019) Identification and Application of Threonine Aldolase for Synthesis of valuable α-amino, β-hydroxy-Building Blocks. Biochimica et Biophysica Acta - Proteins and Proteomics .

Abstract

Chiral β-hydroxy α-amino acid structural motifs are interesting and common synthons present in multiple APIs and drug candidates. To access those chiral building blocks either multistep chemical synthesis is required or advantage can be taken from using threonine aldolases which catalyse aldol reaction between an aldehyde and glycine in a stereoselective way. Bioinformatics tools have been utilized to identify the gene of threonine aldolase from C. humicola and prepare its recombinant version from E. coli fermentation. This enzyme was planned to be implemented as a key step in the synthesis of API. Beside this application, aldolase was purified, characterized and further substrate scope of this enzyme was also investigated. Handful of enzymatic reactions was scale up and products were recovered to access the diastereoselectivity and scaleability of this assymetric synthetic approach towards β-hydroxy α-amino acid chiral building blocks.

Item Type: Article
Keywords: biocatalysis, threonine aldolase, enzymatic synthesis, amino acids, in-silico gene mining
Date Deposited: 10 Dec 2019 00:45
Last Modified: 10 Dec 2019 00:45
URI: https://oak.novartis.com/id/eprint/40408

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