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Record W2323775746 · doi:10.1158/0008-5472.fbcr09-c40

Abstract C40: Salicylic acid-based small molecule inhibitors of Stat3 show potent and selective activity in a variety of human cancer cell lines

2009· article· en· W2323775746 on OpenAlexaff
Brent D. G. Page, Steven Fletcher, Aaron D. Schimmer, James Turkson, Patrick T. Gunning

Bibliographic record

VenueCancer Research · 2009
Typearticle
Languageen
FieldChemistry
TopicSynthesis and biological activity
Canadian institutionsPrincess Margaret Cancer CentreUniversity of Toronto
Fundersnot available
KeywordsSTAT3STAT proteinCancer cellIn vivoCancerActivator (genetics)In vitroBiologyTranscription factorCell cultureCancer researchChemistryApoptosisCell biologyBiochemistryGeneGenetics

Abstract

fetched live from OpenAlex

Abstract Signal transducer and activator of transcription 3 (Stat3) protein is an oncogenic transcription factor that exhibits aberrant functioning in many types human cancer. Constitutive Stat3 activation causes over-expression of anti-apoptotic proteins and makes cancer cells resistant to natural apoptotic processes. Inhibiting Stat3 reduces the expression of anti-apoptotic proteins and can selectively kill cancerous cells. We have identified several salicylic acid based inhibitors of Stat3 that show potent activity in vitro and in whole cell assays. In silico docking studies have revealed S3I-201, a known Stat3 inhibitor, exhibits incomplete occupation of Stat3's SH2 domain. A thorough structure activity relationship study has provided a series of compounds that more completely occupy Stat3's SH2 domain and show potent and highly selective activity against Stat3 and a variety of human cancers. Inhibitor design, synthesis, in vitro and in vivo assays and preliminary metabolic studies will be discussed. Citation Information: Cancer Res 2009;69(23 Suppl):C40.

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 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 score0.110
Threshold uncertainty score0.990

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0010.000
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)0.0000.000

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 head0.082
GPT teacher head0.370
Teacher spread0.288 · 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.

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
Published2009
Admission routes1
Has abstractyes

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