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Record W4400361577 · doi:10.26434/chemrxiv-2024-79nfb

Mechanistic Insights into Cyclodipeptide Formation by Cyclodipeptide Synthases: A Preliminary Exploration on Pathways and Catalytic Residues

2024· preprint· en· W4400361577 on OpenAlexafffund
Akshita Goel, Indu Negi, Ankur Ganesh Pandey, John F. Trant, Purshotam Sharma

Bibliographic record

VenueChemRxiv · 2024
Typepreprint
Languageen
FieldMedicine
TopicPeptidase Inhibition and Analysis
Canadian institutionsUniversity of Windsor
FundersNatural Sciences and Engineering Research Council of CanadaDepartment of Science and Technology, PhilippinesUniversity Grants CommissionDepartment of Science and Technology, Ministry of Science and Technology, India
KeywordsChemistryIntramolecular forceQM/MMCatalysisActive siteStereochemistryEnzymeMolecular dynamicsEnzyme catalysisCombinatorial chemistryComputational chemistryBiochemistry

Abstract

fetched live from OpenAlex

Cyclodipeptide synthases (CDPSs) are enzymes that synthesize cyclodipeptides using two aminoacyl-tRNAs as substrates, but their mechanism remains unclear. This study aims to elucidate the mechanism of AlbC, a CDPS that produces cyclo(L-Phe-L-Phe). We employed small-model quantum mechanics (QM) calculations to propose an intrinsic pathway and molecular dynamics (MD) simulations to identify key catalytic residues involved in this process. The mechanism involves three main steps: activation of Ser37 and the first tRNAPhe to form a Phe-enzyme intermediate, binding of the second tRNAPhe to form a dipeptidyl enzyme intermediate, and intramolecular cyclization to yield the cyclodipeptide. Our QM calculations suggest that Ser37 can be activated through direct transfer of its hydroxyl proton to the O3’ atom of the first substrate. MD simulations highlight the roles of Gly35, Asn40, and His203 in stabilizing the Phe-enzyme intermediate, thus lowering the calculated intrinsic barrier. In the second step, the dipeptidyl enzyme intermediate is favored over the nucleoside intermediate and is stabilized by Asn40, Gln182, and His203 in the AlbC active site, where Gln182 may act as a catalytic base. Additionally, Asn159 and His203 contribute to lowering the significant energy barrier observed in QM calculations for intramolecular cyclization, with Glu182 potentially serving as a catalytic base during this process. Overall, our results support the roles of Asn40 and His203 throughout all mechanistic steps, while highlighting Glu182's involvement in the formation of the dipeptidyl enzyme intermediate and intramolecular cyclization steps. These insights can guide future enzymatic modeling studies of AlbC and potentially other CDPS enzymes using similar approaches.

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 machine prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. The Gemma side is a direct model label for every work in the frame, read from the title-only record. The Codex side is a classifier learned from the 10,348 direct Codex labels and calibrated to design-weighted sample rates; fields without enough sample support carry no Codex call. Candidate is the union of the two sides; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels.

metaresearch head score (Codex)0.000
metaresearch head score (Gemma)0.000
Version: metacan-v3-hybrid-931329e0061cValidation status: machine_predicted_unvalidated
Candidate categoriesnone
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Bench or experimental · Consensus signal: none
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.003
Threshold uncertainty score0.011

Distilled classifier scores by category (both heads)

CategoryCodexGemma
Metaresearch0.0000.000
Meta-epidemiology (narrow)0.0010.000
Meta-epidemiology (broad)0.0000.001
Bibliometrics0.0000.000
Science and technology studies0.0000.000
Scholarly communication0.0010.001
Open science0.0010.000
Research integrity0.0010.001
Insufficient payload (model declined to judge)0.0030.000

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 head0.025
GPT teacher head0.264
Teacher spread0.239 · 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 source (direct Gemma or distilled Codex), 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

Citations0
Published2024
Admission routes2
Has abstractyes

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