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Diversity-Oriented Enzymatic Synthesis of Cyclopropane Building Blocks.

ABSTRACT: While biocatalysis is increasingly incorporated into drug development pipelines, it is less commonly used in the early stages of drug discovery. By engineering a protein to produce a chiral motif with a derivatizable functional handle, biocatalysts can be used to help generate diverse building blocks for drug discovery. Here we show the engineering of two variants of Rhodothermus marinus nitric oxide dioxygenase (RmaNOD) to catalyze the formation of cis- and tran- diastereomers of a pinacolboronate-substituted cyclopropane which can be readily derivatized to generate diverse stereopure cyclopropane building blocks.

SUBMITTER: Wittmann BJ

PROVIDER: S-EPMC7709968 | biostudies-literature | 2020 Jul

REPOSITORIES: biostudies-literature

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Diversity-Oriented Enzymatic Synthesis of Cyclopropane Building Blocks.

Wittmann Bruce J BJ Knight Anders M AM Hofstra Julie L JL Reisman Sarah E SE Kan S B Jennifer SBJ Arnold Frances H FH

ACS catalysis 20200604 13

While biocatalysis is increasingly incorporated into drug development pipelines, it is less commonly used in the early stages of drug discovery. By engineering a protein to produce a chiral motif with a derivatizable functional handle, biocatalysts can be used to help generate diverse building blocks for drug discovery. Here we show the engineering of two variants of Rhodothermus marinus nitric oxide dioxygenase (RmaNOD) to catalyze the formation of cis- and tran- dia ...[more]

PMID: 33282460

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