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Record W2995637865 · doi:10.1172/jci130819

Ivermectin inhibits HSP27 and potentiates efficacy of oncogene targeting in tumor models

2019· article· en· W2995637865 on OpenAlex
Lucia Nappi, A.H. Aguda, Nader Al Nakouzi, Barbara Lelj‐Garolla, Eliana Beraldi, Nada Lallous, Marisa Thi, Susan C. Moore, Ladan Fazli, Dulguun Battsogt, Sophie M. Stief, Fuqiang Ban, Nham T. Nguyen, Neetu Saxena, Evgenia V. Dueva, Fan Zhang, Takeshi Yamazaki, Amina Zoubeidi, Artem Cherkasov, Gary D. Brayer, Martin Gleave

Why this work is in the frame

A frame that forgets how it found something cannot be audited. These are the routes that admitted this work.

affAt least one author lists a Canadian institution in the pinned OpenAlex snapshot.
fundA Canadian funder is recorded on the work.

Bibliographic record

VenueJournal of Clinical Investigation · 2019
Typearticle
Languageen
FieldVeterinary
TopicHelminth infection and control
Canadian institutionsUniversity of British Columbia
FundersNational Institute of General Medical SciencesCanadian Institutes of Health ResearchTerry Fox FoundationMichael Smith Health Research BCProstate Cancer CanadaProstate Cancer Foundation
KeywordsIvermectinOncogenePharmacologyCancer researchHsp27MedicineBiologyImmunologyBioinformaticsHeat shock proteinCancerInternal medicineGeneticsHsp70Cell cycleVeterinary medicineGene

Abstract

fetched live from OpenAlex

HSP27 is highly expressed in, and supports oncogene addiction of, many cancers. HSP27 phosphorylation is a limiting step for activation of this protein and a target for inhibition, but its highly disordered structure challenges rational structure-guided drug discovery. We performed multistep biochemical, structural, and computational experiments to define a spherical 24-monomer complex composed of 12 HSP27 dimers with a phosphorylation pocket flanked by serine residues between their N-terminal domains. Ivermectin directly binds this pocket to inhibit MAPKAP2-mediated HSP27 phosphorylation and depolymerization, thereby blocking HSP27-regulated survival signaling and client-oncoprotein interactions. Ivermectin potentiated activity of anti-androgen receptor and anti-EGFR drugs in prostate and EGFR/HER2-driven tumor models, respectively, identifying a repurposing approach for cotargeting stress-adaptive responses to overcome resistance to inhibitors of oncogenic pathway signaling.

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.

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)0.002
metaresearch head score (Gemma)0.002
Version: codex-gemma-dda1882f352aValidation status: machine_predicted_unvalidated
Candidate categoriesnone
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Observational · Consensus signal: Observational
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.188
Threshold uncertainty score0.317

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0020.002
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 head0.107
GPT teacher head0.387
Teacher spread0.279 · 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