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Record W2069045375 · doi:10.1517/13543776.2011.539205

Signal transducer and activator of transcription 3 inhibitors: a patent review

2010· review· en· W2069045375 on OpenAlex

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.

Bibliographic record

VenueExpert Opinion on Therapeutic Patents · 2010
Typereview
Languageen
FieldMedicine
TopicCytokine Signaling Pathways and Interactions
Canadian institutionsUniversity of Toronto
Fundersnot available
KeywordsSTAT proteinSTAT3RegulatorIn vivoComputational biologySmall moleculePeptidomimeticMedicineCancer researchstatBiologyPharmacologySignal transductionCell biologyPeptideBiochemistryGeneGenetics

Abstract

fetched live from OpenAlex

IMPORTANCE OF THE FIELD: Aberrant activation of signal transducer and activator of transcription (Stat) 3, a member of the STAT family of proteins, is prevalent in numerous human cancers and is now widely recognized as a critical molecular abnormality and a master regulator of tumor processes. Thus, the identification of potent and selective Stat3 inhibitors will have a high commercial potential as anticancer drugs, given the many tumors in which Stat3 is implicated. AREAS COVERED IN THIS REVIEW: This review covers the structures and activities of direct inhibitors of Stat3 protein activity described in the patent literature since the research field's inception in 2001. The patents reviewed include peptide and peptidomimetic compounds, small molecules, oligonucleotides and platinum-based Stat3 inhibitors. WHAT THE READER WILL GAIN: Readers will gain an understanding of how Stat3 protein function has been inhibited by a wide variety of structurally diverse therapeutic compounds. Readers will learn about which classes of patented Stat3 inhibitors are most advanced toward clinical trials, and will be exposed to the proposed mechanisms of inhibition and scope of their application in treating human cancers. TAKE HOME MESSAGE: Numerous groups have shown that in vivo administration of inhibitors of activated Stat3 induce human tumor regression in xenograft models. Indeed, the growing number of preclinical studies in numerous cancer types, as well as the first Phase 0 clinical trial of a Stat3 inhibitor, suggest that Stat3 is a valid and exciting therapeutic target for molecular inhibitors.

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)0.000
metaresearch head score (Gemma)0.000
Version: codex-gemma-dda1882f352aValidation status: machine_predicted_unvalidated
Candidate categoriesMeta-epidemiology (narrow)
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Other design · Consensus signal: none
GenreCandidate signal: Review · Consensus signal: Review
Teacher disagreement score0.977
Threshold uncertainty score1.000

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0000.000
Meta-epidemiology (narrow)0.0010.000
Meta-epidemiology (broad)0.0020.001
Bibliometrics0.0000.000
Science and technology studies0.0000.000
Scholarly communication0.0000.000
Open science0.0000.000
Research integrity0.0000.001
Insufficient payload (model declined to judge)0.0010.000

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 head0.186
GPT teacher head0.390
Teacher spread0.204 · 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