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Record W2513283602 · doi:10.1002/1873-3468.12380

Inhibition of <i>Helicobacter pylori</i> Glu‐t<scp>RNA<sup>G</sup></scp><sup>ln</sup> amidotransferase by novel analogues of the putative transamidation intermediate

2016· letter· en· W2513283602 on OpenAlexafffund
Van Hau Pham, Halim Maaroufi, Christian Balg, Sébastien P. Blais, Nancy Messier, Paul H. Roy, François Otis, Normand Voyer, Jacques Lapointe, Robert Chênevert

Bibliographic record

VenueFEBS Letters · 2016
Typeletter
Languageen
FieldBiochemistry, Genetics and Molecular Biology
TopicRNA and protein synthesis mechanisms
Canadian institutionsCentre hospitalier de l'Université LavalUniversité LavalPROTEO
FundersNatural Sciences and Engineering Research Council of CanadaFonds Québécois de la Recherche sur la Nature et les Technologies
KeywordsGlutamine amidotransferaseHeterotrimeric G proteinChemistryBiochemistryDocking (animal)StereochemistryAmino acidGlutamineMedicineG protein

Abstract

fetched live from OpenAlex

Glutaminyl‐tRNAGln in Helicobacter pylori is formed by an indirect route requiring a noncanonical glutamyl‐tRNA synthetase and a tRNA‐dependent heterotrimeric amidotransferase (AdT) GatCAB. Widespread use of this pathway among prominent human pathogens, and its absence in the mammalian cytoplasm, identify AdT as a target for the development of antimicrobial agents. We present here the inhibitory properties of three dipeptide‐like sulfone‐containing compounds analogous to the transamidation intermediates, which are competitive inhibitors of AdT with respect to Glu‐tRNAGln. Molecular docking revealed that AdT inhibition by these compounds depends on π–π stacking interactions between their aromatic groups and Tyr81 of the GatB subunit. The properties of these inhibitors indicate that the 3′‐terminal adenine of Glu‐tRNAGln plays a major role in binding to the AdT transamidation active site.

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: Bench or experimental
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.002
Threshold uncertainty score0.006

Distilled classifier scores by category (both heads)

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 integrity0.0020.001
Insufficient payload (model declined to judge)0.0020.001

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 head0.009
GPT teacher head0.207
Teacher spread0.198 · 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

Citations7
Published2016
Admission routes2
Has abstractyes

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