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Record W2141447309 · doi:10.1517/14728222.4.4.541

The insulin receptor kinase: modulation and therapeutic implications

2000· article· en· W2141447309 on OpenAlexaff
Barry I. Posner

Bibliographic record

VenueEmerging Therapeutic Targets · 2000
Typearticle
Languageen
FieldChemistry
TopicVanadium and Halogenation Chemistry
Canadian institutionsJewish General HospitalMcGill University
Fundersnot available
KeywordsAutophosphorylationInsulin receptorCell biologyInsulinBiologyPhosphorylationProtein kinase AEndocrinology

Abstract

fetched live from OpenAlex

Following the binding of insulin to its cell surface receptor there is rapid activation of the insulin receptor kinase (IRK), leading to autophosphorylation of the receptor on tyrosine residues and the capacity to tyrosine phosphorylate various cellular substrates. The peroxovanadium compounds (pVs) were shown to activate the IRK in the complete absence of insulin and correlatively activate the full insulin signalling cascade. Along with earlier studies on mutant IRKs, this observation indicated that IRK function is both necessary and sufficient for insulin signaling. IRK is rapidly internalized into the endosomal apparatus (ENs), where it remains activated for a significant time and is capable of entraining insulin signalling events. Thus, modulation of the IRK in ENs is an important means by which insulin signalling is influenced. In recent years, several endosomal processes were shown to regulate IRK activity. The presence in ENs of a relatively specific insulin protease (endosomal acidic insulinase (EAI)) is responsible for limiting ligand availability in this compartment. Also, studies of the mechanism of pV’s ability to activate IRK have identified an IRK-associated PTP (IRK-aPTP) which functions to dephosphorylate and inactivate the activated IRK. Thus, both EAI and IRK-aPTP limit the duration and extent of IRK activation and signalling. Inhibition of IRK-aPTP results in activation of the IRK and the full insulin response. Inhibition of EAI has also been shown to augment IRK activity and signalling. Therefore, EAI and IRK-aPTP are suitable therapeutic targets against which drug development should lead to clinically important agents for treating insulin resistance.

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 categoriesInsufficient payload (model declined to judge)
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Not applicable · Consensus signal: none
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.937
Threshold uncertainty score0.997

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 studies0.0010.000
Scholarly communication0.0000.000
Open science0.0000.000
Research integrity0.0000.000
Insufficient payload (model declined to judge)0.0040.000

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 head0.256
Teacher spread0.241 · 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 designNot applicable
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
Published2000
Admission routes1
Has abstractyes

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