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Record W1988917398 · doi:10.2174/1568006033481375

Selective Protein Kinase C Inhibitors and Their Applications

2003· review· en· W1988917398 on OpenAlex
Garry X. Shen

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

VenueCurrent Drug Targets - Cardiovascular & Hematological Disorders · 2003
Typereview
Languageen
FieldMedicine
TopicCancer Treatment and Pharmacology
Canadian institutionsUniversity of Manitoba
Fundersnot available
KeywordsProtein kinase CGene isoformMedicineClinical trialKinasePharmacologyCancer researchInternal medicineCell biologyBiologyBiochemistry

Abstract

fetched live from OpenAlex

Protein kinase C (PKC) represents a family of phospholipid-dependent serine/threonine kinase. PKC was detected in almost all types of cells and tissues in the body. The activation of PKC is involved in the signal regulation of many physiological and pathological processes. PKC has multiple isoforms (alpha, betaI, betaII, gamma delta, epsilon, eta, theta, xi, iota and micro). PKC-mediated cellular processes are tissue- and isoform-specific. Investigations on selective or isoform-specific PKC inhibitors have attracted great attention during last two decades. Recent studies demonstrated that LY333531, a PKC-beta-specific inhibitor, reduced the development of diabetic vascular complications in animal models and prevented hyperglycemia-induced impairment of endothelial-dependent vasodilation in healthy subjects. Results from phase I clinical trial suggested low risk of the inhibitor. Phase III clinical trials on the safety and the preventive effects of the PKC-beta-specific inhibitor on diabetic complications are under progress. The efficacy of ISSI-3521, a PKC-alpha antisense inhibitor, on slowing the growth and metastasis of solid tumors is currently being examined in clinical trials. Partial responses in the prevention of the progress of malignancies were found in early phases of clinical trials for UCN-01 and CGP41251, two partially isoform-specific PKC inhibitors. Recent findings suggest that isoform-specific PKC inhibitors are potentially beneficial to the prevention or treatment of some common diseases, including cancers and diabetic vascular complications. Safety and efficacy studies of the PKC inhibitors will be required through large-scale long-term clinical trials.

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: Not applicable · Consensus signal: none
GenreCandidate signal: Review · Consensus signal: Review
Teacher disagreement score0.988
Threshold uncertainty score1.000

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0000.000
Meta-epidemiology (narrow)0.0010.001
Meta-epidemiology (broad)0.0040.003
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)0.0000.000

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 head0.030
GPT teacher head0.324
Teacher spread0.293 · 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