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Record W4308373290 · doi:10.15252/emmm.202115200

Blocking STAT3/5 through direct or upstream kinase targeting in leukemic cutaneous T‐cell lymphoma

2022· article· en· W4308373290 on OpenAlexaff
Helena Sorger, Saptaswa Dey, Pablo Vieyra-Garcia, Daniel Pölöske, Andrea Teufelberger, Elvin D. de Araujo, Abootaleb Sedighi, Ricarda Graf, Benjamin Spiegl, Isaac Lazzeri, Till Braun, Ines Garces de los Fayos Alonso, Michaela Schlederer, Gerald Timelthaler, Petra Kodajova, Christine Pirker, Marta Surbek, Michael Machtinger, Thomas Graier, Isabella Perchthaler, Yi Pan, Regina Fink‐Puches, Lorenzo Cerroni, Jennifer Ober, Moritz Otte, Jana D. Albrecht, Gary Tin, Ayah Abdeldayem, Pimyupa Manaswiyoungkul, Olasunkanmi O. Olaoye, Martin Metzelder, Anna Orlova, Walter Berger, Marion Wobser, Jan P. Nicolay, Fiona André, Van Anh Nguyen, Heidi A. Neubauer, Roman Fleck, Olaf Merkel, Marco Herling, Ellen Heitzer, Patrick T. Gunning, Lukas Kenner, Richard Moriggl, Peter Wolf

Bibliographic record

VenueEMBO Molecular Medicine · 2022
Typearticle
Languageen
FieldMedicine
TopicCutaneous lymphoproliferative disorders research
Canadian institutionsUniversity of Toronto
FundersMedizinische Universität GrazAustrian Science FundEuropean Association for Cancer Research
KeywordsCancer researchCutaneous T-cell lymphomaLymphomaSTAT3In vivoBiologyEx vivoT cellLymphoproliferative disordersKinaseMedicineImmunologySignal transductionMycosis fungoidesCell biologyGeneticsImmune system

Abstract

fetched live from OpenAlex

Leukemic cutaneous T-cell lymphomas (L-CTCL) are lymphoproliferative disorders of skin-homing mature T-cells causing severe symptoms and high mortality through chronic inflammation, tissue destruction, and serious infections. Despite numerous genomic sequencing efforts, recurrent driver mutations have not been identified, but chromosomal losses and gains are frequent and dominant. We integrated genomic landscape analyses with innovative pharmacologic interference studies to identify key vulnerable nodes in L-CTCL. We detected copy number gains of loci containing the STAT3/5 oncogenes in 74% (n = 17/23) of L-CTCL, which correlated with the increased clonal T-cell count in the blood. Dual inhibition of STAT3/5 using small-molecule degraders and multi-kinase blockers abolished L-CTCL cell growth in vitro and ex vivo, whereby PAK kinase inhibition was specifically selective for L-CTCL patient cells carrying STAT3/5 gains. Importantly, the PAK inhibitor FRAx597 demonstrated encouraging anti-leukemic activity in vivo by inhibiting tumor growth and disease dissemination in intradermally xenografted mice. We conclude that STAT3/5 and PAK kinase interaction represents a new therapeutic node to be further explored in L-CTCL.

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)0.001
Version: codex-gemma-dda1882f352aValidation status: machine_predicted_unvalidated
Candidate categoriesMeta-epidemiology (narrow), Insufficient payload (model declined to judge)
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 score0.367
Threshold uncertainty score1.000

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0010.001
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0010.000
Bibliometrics0.0000.001
Science and technology studies0.0000.000
Scholarly communication0.0000.000
Open science0.0000.000
Research integrity0.0000.001
Insufficient payload (model declined to judge)0.0030.000

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 head0.019
GPT teacher head0.304
Teacher spread0.286 · 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
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

Citations28
Published2022
Admission routes1
Has abstractyes

Explore more

Same venueEMBO Molecular MedicineSame topicCutaneous lymphoproliferative disorders researchFrench-language works237,207