Identification of a First Enzymatic Activator of a 17β-Hydroxysteroid Dehydrogenase
Bibliographic record
Abstract
Small molecule activators that directly modulate the activity of an enzyme are uncommon entities, and such activators had never yet been identified for any 17β-hydroxysteroid dehydrogenase (17β-HSD). We hereby report the fortuitous discovery of a steroid derivative that caused an up to 3-fold increase in the activity of 17β-HSD12. The stimulation of estrone to estradiol conversion has been characterized in intact and homogenized stably transfected HEK-293 cells and has also been observed in T47D breast cancer cells. Structure-activity relationships closely linked to the nature of the substituent on the [1,3]oxazinan-2-one ring of an estradiol derivative emerged from this study and may help in the identification of a previously unsuspected endogenous activation of 17β-HSD12. This activator will therefore be a useful tool to study this relatively unknown enzyme as well as the possible activation of other 17β-HSD family members.
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How this classification was reachedexpand
Full frame machine prediction
Teacher imitationNot 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.
Distilled classifier scores by category (both heads)
| Category | Codex | Gemma |
|---|---|---|
| Metaresearch | 0.000 | 0.000 |
| Meta-epidemiology (narrow) | 0.000 | 0.000 |
| Meta-epidemiology (broad) | 0.000 | 0.000 |
| Bibliometrics | 0.000 | 0.000 |
| Science and technology studies | 0.000 | 0.000 |
| Scholarly communication | 0.000 | 0.000 |
| Open science | 0.000 | 0.000 |
| Research integrity | 0.000 | 0.001 |
| Insufficient payload (model declined to judge) | 0.002 | 0.001 |
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.
score_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from itClassification
machine, unvalidatedMachine predicted; a candidate call from one source (direct Gemma or distilled Codex), not a consensus.
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".