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DEPTOR Tyrosine Phosphorylation: A Novel Molecular Switch Involved in mTOR Activity

2021· article· en· W3172886798 on OpenAlexafffund
Laurence M. Gagné, Nadine Morin, Noémie Lavoie, Jean‐Philippe Lambert, Nicolas Bisson, Frédérick A. Mallette, Marc‐Étienne Huot

Bibliographic record

VenueThe FASEB Journal · 2021
Typearticle
Languageen
FieldBiochemistry, Genetics and Molecular Biology
TopicPI3K/AKT/mTOR signaling in cancer
Canadian institutionsUniversité LavalUniversité du Québec à MontréalCentre hospitalier de l'Université LavalUniversité de MontréalCentre hospitalier universitaire de Québec
FundersCancer Research Society
KeywordsmTORC1PI3K/AKT/mTOR pathwaymTORC2PhosphorylationCancer researchTyrosine phosphorylationCell biologyRPTORReceptor tyrosine kinaseTyrosineChemistryProtein kinase BTyrosine kinaseSH2 domainBiologySignal transductionBiochemistry

Abstract

fetched live from OpenAlex

Dysregulated mTOR (mechanistic Target Of Rapamycin) is a potent tumor growth inducer known to promote cancer cell proliferation and survival. Its activity can be regulated by numerous factors composing the PTEN/PI3K/AKT canonical pathway, which are often mutated in cancer. However, in a subset of cancer showing a constitutively activated mTOR, there is no alteration within the canonical activation pathway, suggesting different activation mechanism. We previously discovered several post‐translational modifications (PTMs) on DEP domain‐containing mTOR‐interacting protein (DEPTOR), an endogenous regulator of the two mTOR complexes (mTORC1 and mTORC2). Still, the mechanism by which these PTMs regulate DEPTOR ability to shut down mTOR complexes remains ill‐defined. Studies have only shown that DEPTOR is phosphorylated on serine (S286/287/291/293/299) under high energy level condition, leading to its degradation by the ubiquitin/proteasome system. Unlike this irreversible regulatory mechanism, we have recently identified another PTM, a tyrosine phosphorylation that affects DEPTOR inhibitory functions. We found that phosphorylation of DEPTOR tyrosine 289 increase its stability, while promoting DEPTOR dissociation from mTORC1&2, leading to a rapid and sustain increase in mTORC1&2 activity. To identify the upstream signaling pathway causing tyrosine 289 phosphorylation, we performed mass spectrometry analysis, as well as a small drug screening of different tyrosine kinase inhibitors. Using these combined methods, we identify Syk (Spleen tyrosine kinase), whose expression levels correlate with levels of tyrosine 289 phosphorylation. We also found that Syk‐induced phosphorylation of DEPTOR was regulated by the EphB2 receptor. Our findings uncovered a new mechanism regulating mTOR activity, which explains the increased mTOR activity in cancer with unaffected PTEN/PI3K/AKT regulatory pathways. Better understanding of this mTOR/DEPTOR regulatory pathway could allow the development of a new therapeutic approach to inhibit mTOR associated cancer progression.

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 score0.004

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 head0.017
GPT teacher head0.259
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 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

Citations0
Published2021
Admission routes2
Has abstractyes

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