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Transaminases for the synthesis of enantiopure beta-amino acids

机译:转氨酶用于合成对映纯的β-氨基酸

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摘要

Optically pure β-amino acids constitute interesting building blocks for peptidomimetics and a great variety of pharmaceutically important compounds. Their efficient synthesis still poses a major challenge. Transaminases (also known as aminotransferases) possess a great potential for the synthesis of optically pure β-amino acids. These pyridoxal 5'-dependent enzymes catalyze the transfer of an amino group from a donor substrate to an acceptor, thus enabling the synthesis of a wide variety of chiral amines and amino acids. Transaminases can be applied either for the kinetic resolution of racemic compounds or the asymmetric synthesis starting from a prochiral substrate. This review gives an overview over microbial transaminases with activity towards β-amino acids and their substrate spectra. It also outlines current strategies for the screening of new biocatalysts. Particular emphasis is placed on activity assays which are applicable to high-throughput screening.
机译:光学纯的β-氨基酸构成了拟肽和多种药学上重要的化合物的重要组成部分。它们的有效合成仍然是一个重大挑战。转氨酶(也称为氨基转移酶)具有合成光学纯β-氨基酸的巨大潜力。这些依赖吡咯醛的5'依赖性酶催化氨基从供体底物向受体的转移,从而能够合成多种手性胺和氨基酸。转氨酶可用于外消旋化合物的动力学拆分或从前手性底物开始的不对称合成。这篇综述概述了对β-氨基酸具有活性的微生物转氨酶及其底物谱。它还概述了筛选新生物催化剂的当前策略。特别强调适用于高通量筛选的活性测定法。

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