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Record W2790811214 · doi:10.1093/jcag/gwy008.314

A313 MUCOSAL PROTEASES FROM IBS PATIENTS PRODUCE LONG TERM HYPEREXCITABILITY IN NOCICEPTIVE DRG NEURONS BY ACTIVATING NOVEL INTRACELLULAR SIGNALING PATHWAYS

2018· article· en· W2790811214 on OpenAlexaff
Nestor N. Jiménez-Vargas, David E. Reed, Nigel W. Bunnett, S Vanner

Bibliographic record

VenueJournal of the Canadian Association of Gastroenterology · 2018
Typearticle
Languageen
FieldPharmacology, Toxicology and Pharmaceutics
TopicAdvanced Drug Delivery Systems
Canadian institutionsKingston General HospitalQueen's University
Fundersnot available
KeywordsRheobaseProteasesNociceptionIrritable bowel syndromeReceptorPharmacologyMedicineNeuroscienceChemistryInternal medicineCell biologyBiologyElectrophysiologyBiochemistryEnzyme

Abstract

fetched live from OpenAlex

Patients suffering from the irritable bowel syndrome report exaggerated and sustained abdominal pain. We have shown that activation of protease activated receptor 2 (PAR2) on nociceptive (pain sensing) dorsal root ganglia (DRG) neurons evoke long term hyperexcitability but the mechanisms of this sustained pain signaling are unclear. Recent studies show that trypsin activates canonical PAR2 signaling causing endocytosis and this leads to sustained PAR2- endosomal signaling. Proteases such as elastase and cathepsin S, however, act at non-canonical sites and do not cause receptor endocytosis. We have shown that protease activity is increased in IBS tissues but it is unclear whether this leads to sustained neuronal excitation. To examine whether proteases in tissues from IBS patients lead to sustained nociceptive signaling and, if so, what intracellular mechanisms are involved. DRG neurons (T9-T13) from C57BL/6 mice were pre-incubated (10 min) with Trypsin (50nM) or supernatants (30 min) from colonic biopsies obtained from diarrhea predominant IBS patients or controls then washed with F12 media. We measured neuronal excitability by perforated patch-clamp, recording changes in rheobase (minimum current to fire action potential) and action potential discharged at twice rheobase immediately after washing with F12 media (time 0) or ~ 30 min later (time 30). PAR2 (10 μM I-343) and ERK1/2 (50 μM PD8059) inhibitors were applied 30 min before IBS supernatant or trypsin. Two way ANOVA and post hoc Tuckey’s tests were used to analyze the data. IBS supernatants increased DRG neuronal excitability acutely (time 0) as well as sustained hyperexcitability (time 30) (Table 1). This was blocked by the PAR2 antagonist I-343. This sustained excitability was also blocked by antagonist of ERK1/2. Sustained excitability evoked by trypsin was also inhibited by the ERK1/2 antagonist. Proteases in IBS tissues, acting through PAR2, evoke long term hyperexcitability of nociceptive signaling in DRG neurons that is ERK1/2 dependent. In addition, the sustained excitability evoked by the serine protease trypsin, which we previously have shown is mediated by PAR2-endosomal signaling, was also ERK1/2 dependent. Thus, serine proteases in IBS tissues may be signaling through similar pathways and these could provide a novel therapeutic target to treat pain in patients with IBS. CAGCONACYT

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)0.001
metaresearch head score (Gemma)0.002
Version: codex-gemma-dda1882f352aValidation status: machine_predicted_unvalidated
Candidate categoriesnone
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Observational · Consensus signal: Observational
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.065
Threshold uncertainty score0.949

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0010.002
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 integrity0.0000.001
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 head0.039
GPT teacher head0.310
Teacher spread0.271 · 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 designObservational
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
Published2018
Admission routes1
Has abstractyes

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