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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 OpenAlexaff
A Ata

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.

How this classification was reachedexpand

Full frame machine prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. The Gemma side is a direct model label for every work in the frame, read from the title-only record. The Codex side is a classifier learned from the 10,348 direct Codex labels and calibrated to design-weighted sample rates; fields without enough sample support carry no Codex call. Candidate is the union of the two sides; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels.

metaresearch head score (Codex)0.000
metaresearch head score (Gemma)0.000
Version: metacan-v3-hybrid-931329e0061cValidation 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 score0.003
Threshold uncertainty score0.009

Distilled classifier scores by category (both heads)

CategoryCodexGemma
Metaresearch0.0000.000
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0000.000
Bibliometrics0.0010.000
Science and technology studies0.0000.000
Scholarly communication0.0000.000
Open science0.0000.000
Research integrity0.0000.001
Insufficient payload (model declined to judge)0.0030.001

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

Classification

machine, unvalidated

Machine predicted; a candidate call from one source (direct Gemma or distilled Codex), 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
Published2014
Admission routes1
Has abstractyes

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