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Diversity-Oriented Enzymatic Synthesis of Cyclopropane Building Blocks

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posted on 17.06.2020 by Bruce J. Wittmann, Anders M. Knight, Julie L. Hofstra, Sarah E. Reisman, S. B. Jennifer Kan, Frances H. Arnold
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 trans-diastereomers of a pinacolboronate-substituted cyclopropane which can be readily derivatized to generate diverse stereopure cyclopropane building blocks.

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