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Record W4245513075 · doi:10.1385/0-89603-519-0:153

Thin-Layer Chromatographic Analysis of Human CYP3A-Catalyzed Testosterone 6P-Hydroxylation

2003· book-chapter· en· W4245513075 on OpenAlexaff
David J. Waxman, Thomas K. H. Chang

Bibliographic record

VenueHumana Press eBooks · 2003
Typebook-chapter
Languageen
FieldPharmacology, Toxicology and Pharmaceutics
TopicPharmacogenetics and Drug Metabolism
Canadian institutionsUniversity of British Columbia
FundersNational Institute of Diabetes and Digestive and Kidney Diseases
KeywordsCYP3ACYP3A4MicrosomeCytochrome P450BiologyHydroxylationTestosterone (patch)ChemistryEnzymeBiochemistryMolecular biologyEndocrinology

Abstract

fetched live from OpenAlex

At least two cytochromes P450 belonging to the CYP3A subfamily may be expressed in adult human liver ( 1 ), CYP3A4 and CYP3A5. A third enzyme, CYP3A7, is expressed in human fetal liver ( 2 ). The CYP3A enzymes account for an estimated ~30% of total human cytochrome P450 content in adult liver ( 3 ), although large inter-individual differences exist in hepatic CYP3A content. CYP3A4 is present in all adult human livers and is inducible by drugs such as rifampin (rifampicin) and dexamethasone ( 4 – 6 ). By contrast, CYP3A5 is expressed in only ~ 10-30% of liver samples ( 7 ) and does not respond to typical CYP3A inducers ( 5 , 6 ). Triacetyloleandomycin ( 8 , 9 ) and gestodene ( 9 ) are CYP3A-selective chemical inhibitors. Many commonly used drugs are substrates for CYP3A, including erythromycin ( 10 ), infedipine ( 11 ) and midazolam ( 12 ). Immunoinhibition experiments with CYP3A subfamily-specific antibodies have established several microsomal enzyme activities, including nifedipine oxidase ( 11 , 13 ) and testosterone 6β-hydroxylase ( 14 , 15 ), as useful catalytic monitors for hepatic CYP3A In a recent study, an inhibitory antipeptide antibody against CYP3A4, which did not cross-react with cDNA-expressed CYP3A5 as judged by Western-blot analysis and did not inhibit cDNA-expressed CYP3A5-catalyzed testosterone 6β-hydroxylation, was found to inhibit virtually all of the testosterone 6β-hydroxylase activity in human liver microsomes ( 16 ), suggesting that this activity has a high specificity for hepatic CYP3A4.

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)0.001
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 score0.004
Threshold uncertainty score0.014

Distilled classifier scores by category (both heads)

CategoryCodexGemma
Metaresearch0.0000.001
Meta-epidemiology (narrow)0.0010.000
Meta-epidemiology (broad)0.0010.001
Bibliometrics0.0020.001
Science and technology studies0.0010.000
Scholarly communication0.0000.000
Open science0.0000.000
Research integrity0.0010.001
Insufficient payload (model declined to judge)0.0040.002

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 head0.212
GPT teacher head0.415
Teacher spread0.203 · 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
Published2003
Admission routes1
Has abstractyes

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