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Record W4393073512 · doi:10.1038/s41467-024-46559-3

Diindoles produced from commensal microbiota metabolites function as endogenous CAR/Nr1i3 ligands

2024· article· en· W4393073512 on OpenAlexafffund
Jiabao Liu, Ainaz Malekoltojari, Anjana Asokakumar, Vimanda Chow, Linhao Li, Hao Li, Marina Grimaldi, Nathanlown Dang, Jhenielle Campbell, Holly Barrett, Jianxian Sun, William Wiley Navarre, Derek J. Wilson, Hongbing Wang, Sridhar Mani, Patrick Balaguer, Sayeepriyadarshini Anakk, Henry M. Krause

Bibliographic record

VenueNature Communications · 2024
Typearticle
Languageen
FieldPharmacology, Toxicology and Pharmaceutics
TopicPharmacogenetics and Drug Metabolism
Canadian institutionsYork UniversityUniversity of Toronto
FundersNational Institute of Diabetes and Digestive and Kidney DiseasesNatural Sciences and Engineering Research Council of CanadaUniversity of Illinois at Urbana-ChampaignCanadian Institutes of Health ResearchAmerican Cancer SocietyCanadian Network for Research and Innovation in Machining Technology, Natural Sciences and Engineering Research Council of CanadaNational Cancer InstituteNational Institutes of HealthU.S. Department of Health and Human ServicesGovernment of CanadaAgence Nationale de la Recherche
KeywordsNuclear receptorMicrobiomeBiologyHuman microbiomeComputational biologyFunction (biology)BacteriaReceptorHost (biology)GeneCell biologyGeneticsTranscription factor

Abstract

fetched live from OpenAlex

Numerous studies have demonstrated the correlation between human gut bacteria and host physiology, mediated primarily via nuclear receptors (NRs). Despite this body of work, the systematic identification and characterization of microbe-derived ligands that regulate NRs remain a considerable challenge. In this study, we discover a series of diindole molecules produced from commensal bacteria metabolites that act as specific agonists for the orphan constitutive androstane receptor (CAR). Using various biophysical analyses we show that their nanomolar affinities are comparable to those of synthetic CAR agonists, and that they can activate both rodent and human CAR orthologues, which established synthetic agonists cannot. We also find that the diindoles, diindolylmethane (DIM) and diindolylethane (DIE) selectively up-regulate bona fide CAR target genes in primary human hepatocytes and mouse liver without causing significant side effects. These findings provide new insights into the complex interplay between the gut microbiome and host physiology, as well as new tools for disease treatment.

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 score0.001
Threshold uncertainty score0.005

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 integrity0.0000.000
Insufficient payload (model declined to judge)0.0010.000

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 head0.119
GPT teacher head0.431
Teacher spread0.312 · 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

Citations18
Published2024
Admission routes2
Has abstractyes

Explore more

Same venueNature Communications→Same topicPharmacogenetics and Drug Metabolism→French-language works237,207→