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Record W2326038632 · doi:10.1055/s-0034-1382612

Novel enzyme inhibiting natural products from medicinally important plants

2014· article· en· W2326038632 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

VenuePlanta Medica · 2014
Typearticle
Languageen
FieldBiochemistry, Genetics and Molecular Biology
TopicEnzyme function and inhibition
Canadian institutionsUniversity of Winnipeg
Fundersnot available
KeywordsNatural productEnzymeDrug discoveryBiochemistryBiologyComputational biologyPharmacology

Abstract

fetched live from OpenAlex

Natural products derived from plants, marine organisms and microorganisms exhibit interesting anti-microbial, anti-viral, and anti-inflammatory activities. These bioactivities make natural products an important source for the discovery of new pharmaceutical agents, and more than 60% of the drugs available on the market are of natural product origin. One of the aspects of drug discovery process is the identification of small molecules with enzyme-inhibiting activities. Enzymes are essential to human life, mediating biochemical processes including metabolism, cellular signal transduction, cell cycling, and development. Malfunction in these biochemical systems often leads to disease that can be caused either by the dysfunction, overexpression, or hyper-activation of the enzymes involved. An understanding of diseases at the molecular level has provided several enzyme inhibitors in clinics. For instance, galanthamine, a potent acetylcholinesterase (AChE) inhibitor, is used to treat Alzheimer's disease. In-vitro enzyme inhibition assays can easily be performed in any natural product chemistry lab in order to discover lead compounds against various biological targets. For instance, glutathione S-transferase (GST) inhibitors have applications in overcoming the drug resistance problems in cancer and parasite chemotherapy. Fatty acid synthase inhibitors are used to discover anti-malarial, anti-parasitic, anti-TB and anti-fungal compounds. We are involved in discovering new enzyme inhibitors from medicinally important plants. These efforts have resulted in the identification of a few novel AChE, GST and α-glucosidase inhibitors. During this presentation, structure elucidation of these new enzyme inhibitors and their bioactivity data will be discussed. Additionally, results obtained from structure-activity relationship studies will also be presented.

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)0.001
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 score0.082
Threshold uncertainty score0.563

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0000.001
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 head0.009
GPT teacher head0.218
Teacher spread0.209 · 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