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Record W2101090893 · doi:10.1517/14728222.2015.1042365

Subcellular G-protein coupled receptor signaling hints at greater therapeutic selectivity

2015· editorial· en· W2101090893 on OpenAlexafffund
Jean‐Sébastien Joyal, Vikrant K. Bhosle, Sylvain Chemtob

Bibliographic record

VenueExpert Opinion on Therapeutic Targets · 2015
Typeeditorial
Languageen
FieldBiochemistry, Genetics and Molecular Biology
TopicReceptor Mechanisms and Signaling
Canadian institutionsHôpital Maisonneuve-RosemontUniversité de MontréalMcGill UniversityCentre Hospitalier Universitaire Sainte-Justine
FundersCanadian Institutes of Health Research
KeywordsG protein-coupled receptorReceptorSubcellular localizationCell biologySignal transductionNucleusBiologyExtracellularRhodopsin-like receptorsCell surface receptorIntracrineTransmembrane proteinCellFunctional selectivityCytoplasmBiochemistryAgonistParacrine signalling

Abstract

fetched live from OpenAlex

G-protein coupled receptors (GPCRs) evolved as specialized sensors of the extracellular environment. Comprising the largest family of cell surface receptors, GPCRs are common therapeutic targets. Over the last 25 years, several GPCRs have been observed at the cell nucleus, suggesting the presence of intracrine GPCR signaling beyond the plasma membrane. Yet specific physiological functions of nuclear GPCRs had not been reported, until lately. We recently uncovered distinct but complementary angiogenic roles of F2rl1 (formerly known as PAR2) depending on its subcellular localization at the plasma membrane or at the nucleus. Targeting subcellular compartments to improve drug selectivity may therefore inspire novel therapeutic strategies for transmembrane receptors.

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)0.000
Version: codex-gemma-dda1882f352aValidation status: machine_predicted_unvalidated
Candidate categoriesMeta-epidemiology (narrow), Research integrity, Insufficient payload (model declined to judge)
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Bench or experimental · Consensus signal: none
GenreCandidate signal: Editorial · Consensus signal: Editorial
Teacher disagreement score0.284
Threshold uncertainty score1.000

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0010.000
Meta-epidemiology (narrow)0.0010.001
Meta-epidemiology (broad)0.0010.000
Bibliometrics0.0000.000
Science and technology studies0.0000.000
Scholarly communication0.0000.000
Open science0.0010.000
Research integrity0.0020.001
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 head0.023
GPT teacher head0.282
Teacher spread0.258 · 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.

Study designBench or experimental
Domainnot available
GenreEditorial

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

Citations24
Published2015
Admission routes2
Has abstractyes

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