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The role of MCT1 and MCT4 in drug‐induced muscle disorders

2013· article· en· W38214635 on OpenAlexaff
Yat Hei Leung, Jennifer Lu, M. Papillon, François Bélanger, Jacques Turgeon, Véronique Michaud

Bibliographic record

VenueThe FASEB Journal · 2013
Typearticle
Languageen
FieldMedicine
TopicPharmacological Effects and Toxicity Studies
Canadian institutionsUniversité de Montréal
Fundersnot available
KeywordsLactic acidChemistryFluvastatinPharmacologyIntracellularCerivastatinAtorvastatinBiochemistrySimvastatinMedicineCholesterolBiology

Abstract

fetched live from OpenAlex

Background Muscle injury, including myopathy, is a common side effect of some drugs, and particularly of statins. We hypothesized that these side effects are related to intracellular accumulation of lactic acid through monocarboxylate transporters, MCT1 and MCT4. Our objective was to investigate whether the transport of lactic acid is modulated by statins and other acidic drugs. Methods Cell lines used as models for MCT1 and MCT4 were Hs578T and MDA‐MB‐231, respectively. The cells were incubated with [ 14 C]lactic acid at 37°C and the intracellular concentration of radioactive lactic acid was measured. Inhibition studies were conducted by co‐incubating the cells with different concentrations of acidic drugs (e.g. statins, gemfibrozil, irbesartan, losartan, valsartan, loratadine, ibuprofen, naproxen, and salicylic acid) and lactic acid. Results Atorvastatin and loratadine showed the highest inhibition with IC 50 of 20 μM and 2μM, respectively. Fluvastatin and irbesartan showed an intermediate inhibition with IC 50 of 100–1000 μM, while drugs such as lovastatin and NSAID showed low or no inhibition (IC 50 >;1000 μM). Conclusions These results imply that atorvastatin and other acidic drugs can lead to the accumulation of lactic acid due to the blockage of MCT1 and MCT4. Further studies are required to link the intracellular accumulation of lactic acid and drug‐induced muscle pain. Research supports; CIHR and HSF

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: Observational · Consensus signal: none
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.879
Threshold uncertainty score0.154

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0000.000
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0000.000
Bibliometrics0.0000.000
Science and technology studies0.0000.000
Scholarly communication0.0000.000
Open science0.0000.000
Research integrity0.0000.000
Insufficient payload (model declined to judge)0.0000.000

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 head0.011
GPT teacher head0.264
Teacher spread0.253 · 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

Citations5
Published2013
Admission routes1
Has abstractyes

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