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Record W4396818181 · doi:10.1107/s2053273323087818

Structural biology of glucose-6-phosphate dehydrogenase and small-molecule activators

2023· article· en· W4396818181 on OpenAlexaff
Claire M. Weekley, Agnes Wong, Michael W. Parker, Lindsay E. Wu

Bibliographic record

VenueActa Crystallographica Section A Foundations and Advances · 2023
Typearticle
Languageen
FieldMedicine
TopicNeonatal Health and Biochemistry
Canadian institutionsDiscovery Centre
Fundersnot available
KeywordsSmall moleculeGlucose-6-phosphate dehydrogenaseDehydrogenaseBiochemistryChemistryBiologyEnzyme

Abstract

fetched live from OpenAlex

Glucose-6-phosphate dehydrogenase (G6PD) is a rate-limiting enzyme in the pentose phosphate pathway.It's essential for the production of NADPH and glutathione, and the reduction of reactive oxygen species.G6PD exists as inactive monomers and active dimers and tetramers, with its structure and activity sensitive to the presence of its co-factors NADP+ and glucose-6phosphate.G6PD deficiency is one of the most common enzymatic disorders, with over 150 single mutations known to affect enzyme activity.G6PD activity also declines with age and is associated with the accumulation of oxidative DNA damage [1].By contrast, increased G6PD activity has been shown to extend lifespan and healthspan in animal models [2].Overcoming G6PD decline and deficiency with the use of activators may help prevent diseases of ageing and treat hereditary G6PD deficiency.Indeed, novel small molecule activators of G6PD increase the lifespan of worms.Here, we explore the mechanisms by which small molecules activate G6PD using X-ray crystallography, analytical size exclusion chromatography and HDX-MS.It was hypothesised that these molecules stabilise G6PD in its more active tetrameric state.However, we've found that these small molecule activators do not alter the oligomeric state of G6PD in solution.Instead, X-ray crystallography reveals a paradox where the soaking of a small molecule activator into the crystals results into the loss of density for structural NADP+, which is usually associated with reduced G6PD activity [3,4].

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: none
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.613
Threshold uncertainty score0.377

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0000.000
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0000.000
Bibliometrics0.0000.001
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 head0.015
GPT teacher head0.294
Teacher spread0.280 · 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

Citations0
Published2023
Admission routes1
Has abstractyes

Explore more

Same venueActa Crystallographica Section A Foundations and AdvancesSame topicNeonatal Health and BiochemistryFrench-language works237,207