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Record W2970250436 · doi:10.1002/cctc.201901200

Customizing the Enantioselectivity of a Cyclohexanone Monooxygenase by a Strategy Combining “Size‐Probes” with <i>in silico</i> Study

2019· article· en· W2970250436 on OpenAlexfundno aff
Yujing Hu, Jian Xu, Yixin Cen, Danyang Li, Yu Zhang, Meilan Huang, Xianfu Lin, Qi Wu

Bibliographic record

VenueChemCatChem · 2019
Typearticle
Languageen
FieldBiochemistry, Genetics and Molecular Biology
TopicEnzyme Catalysis and Immobilization
Canadian institutionsnot available
FundersFundamental Research Funds for the Central UniversitiesNatural Science Foundation of Zhejiang ProvinceQueen's UniversityNational Natural Science Foundation of ChinaQueen's University Belfast
KeywordsIn silicoCyclohexanoneRational designCombinatorial chemistryChemistryMonooxygenaseDirected evolutionMutantSmall moleculeProtein engineeringStereochemistryEnzymeCatalysisNanotechnologyBiochemistryMaterials scienceCytochrome P450Gene

Abstract

fetched live from OpenAlex

Abstract Enzymatic Baeyer‐Villiger oxidation provides a promising green route utilizing molecular oxygen as the oxidant to produce chiral lactones. Wild‐type (WT) CHMO Acineto leads to enantioselectivity up to 99 % ee ( S ) in the synthesis of substituted ϵ‐caprolactones. To reverse the inherent enantiopreference of CHMO Acineto toward an array of cyclohexanones with various chain length, we herein reshaped the binding pocket with a minimal number of mutations by a rational design strategy combining “size‐probes” with in silico study, which drastically reduces the screening effort. By probing the binding pocket of variants with different‐sized 4‐substituted cyclohexanones substrates, single, double and triple mutants were identified as the best mutants providing highly reversed enantioselectivity for these probing molecules, respectively. The successful demonstration of the strategy combining “size‐probes” with in silico study in the protein engineering of CHMO Acineto may provide a valuable guidance for facile engineering other BVMOs with customized enantiopreference for the same classified substrates with their substituents on the chiral or prochiral central atom.

Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.

How this classification was reachedexpand

Full frame distilled prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.

metaresearch head score (Codex)0.000
metaresearch head score (Gemma)0.000
Version: codex-gemma-dda1882f352aValidation status: machine_predicted_unvalidated
Candidate categoriesnone
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Bench or experimental · Consensus signal: Bench or experimental
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.024
Threshold uncertainty score0.480

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0000.000
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0000.000
Bibliometrics0.0000.000
Science and technology studies0.0000.000
Scholarly communication0.0000.000
Open science0.0000.000
Research integrity0.0000.000
Insufficient payload (model declined to judge)0.0000.000

Machine scores (provisional)

The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.

Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.

Opus teacher head0.005
GPT teacher head0.217
Teacher spread0.212 · how far apart the two teachers sit on this one work
Validation statusscore_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it

Classification

machine, unvalidated

Machine predicted; a candidate call from one teacher head, not a consensus.

The models applied no category: nothing in the taxonomy fit this work.
Study designBench or experimental
Domainnot available
GenreEmpirical

How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".

Quick stats

Citations3
Published2019
Admission routes1
Has abstractyes

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