From Computational Screening to Preparative Scale: A Transaminase Identified by Machine Learning for (R)-1-Boc-3-aminopyrrolidine

Engineering an (R)-Selective Transaminase for High-Substrate-Loading Asymmetric Amination of a Sterically Demanding N-Heterocyclic Ketone.

The biocatalytic asymmetric amination of bulky N-heterocyclic ketones is often limited by low enzyme activity and poor performance at high substrate loading. Herein, we developed an efficient (R)-selective transaminase for the synthesis of (R)-1-Boc-3-aminopiperidine through an integrated strategy combining phylogeny-g...

Creating a non-native bio-amidation activity in asparagine synthetase via biosensor-guided directed evolution for the synthesis of (S)-2-aminobutyramide

The direct asymmetric synthesis of chiral amides remains a focal point in green manufacturing, particularly for (S)-2-aminobutyramide whose traditional production is often hampered by low atom economy and arduous chiral resolution steps. Here, we report the creation of a non-native bio-amidation activity in Escherichia...

[Directed evolution of amine dehydrogenase for the catalytic resolution of (1R,5S)-3-ethylbicyclo [3.2.0] hept-3-en-6-one, a chiral intermediate of mirogabalin].

Discovery and evolution of an (R)-selective transaminase for production of sitagliptin

R reverse screening as an effective approach for evolving transaminases toward sterically hindered substrates is validates reverse screening as an effective approach for evolving transaminases toward sterically hindered substrates and highlights RTA-223 as a promising candidate for further biocatalyst development.

Mechanochemical Synthesis, Characterization, and Biological Evaluation of N-Cyclohexyl-1,2,3,4-tetrahydro-pyrimidine-5-carboxamide Derivatives

Chemical Rescue Serves as a Predictive Proxy for Glycosynthase Activity on Glycosidic Bonds via a Shared Glycosyl Oxocarbenium Transition State

It is demonstrated that chemical rescue—the azide-mediated restoration of hydrolytic activity in nucleophile-deficient mutants—serves as a predictive, high-throughput proxy for glycosynthase activity as well as a structural and thermodynamic rationale for using CR to select for transition-state-stabilizing mutations.