Repertoire of Computationally Designed Peroxygenases for Enantiodivergent C¿H Oxyfunctionalization Reactions

[EN] The generation of enantiodivergent biocatalysts for C-H oxyfunctionalisations is ever more important in modern synthetic chemistry. Here, we have applied the FuncLib algorithm based on phylogenetic and Rosetta calculations to design a diverse repertoire of active, stable and enantiodivergent fu...

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Detalles Bibliográficos
Autores: Gómez de Santos, Patricia, Mateljak, Ivan, Hoang, Manh Dat, Fleishman, Sarel J., Hollmann, Frank, Alcalde Galeote, Miguel
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2023
País:España
Institución:Consejo Superior de Investigaciones Científicas (CSIC)
Repositorio:DIGITAL.CSIC. Repositorio Institucional del CSIC
OAI Identifier:oai:digital.csic.es:10261/343651
Acceso en línea:http://hdl.handle.net/10261/343651
Access Level:acceso abierto
Palabra clave:Unspecific peroxygenase
Enantiodivergence
C-H oxyfunctionalisation
FuncLib
Computational protein design
Directed evolution.
Descripción
Sumario:[EN] The generation of enantiodivergent biocatalysts for C-H oxyfunctionalisations is ever more important in modern synthetic chemistry. Here, we have applied the FuncLib algorithm based on phylogenetic and Rosetta calculations to design a diverse repertoire of active, stable and enantiodivergent fungal peroxygenases. 24 designs, each carrying 4-5 mutations in the catalytic core, were expressed functionally in yeast and benchmarked against characteristic model compounds. Several designs were active and stable in a range of temperature and pH, displaying unprecedented enantiodivergence, changing regioselectivity from alkyl to aromatic hydroxylation, and increasing catalytic efficiencies up to 10-fold, with 15-fold improvements in total turnover numbers over parental enzyme. We find that this dramatic functional divergence stems from beneficial epistasis among the mutations and an extensive reorganization of the heme channel. Our work demonstrates that FuncLib can rapidly design highly functional libraries enriched in enantioselective peroxygenases not seen in nature for a range of biotechnological applications.