An overview of patented small molecule stearoyl coenzyme-A desaturase inhibitors (2009 – 2013)
Bibliographic record
Abstract
INTRODUCTION: Stearoyl coenzyme-A desaturase (SCD) is a critical lipogenic enzyme that converts a range of unsaturated lipids to their corresponding monounsaturated fatty acids. Genetic and enzyme-knockdown experiments have suggested an important role of SCD1 in the regulation of various metabolic disorders. With the prognostication that SCD-inhibition may serve to remediate various metabolic diseases, several pharmaceutical companies have embarked on the development of small-molecule SCD-inhibitors, with over 100 patent applications by 17 companies being reported to date. AREAS COVERED: Recent progress on the development of SCD-inhibitors, including preclinical efficacy and safety are reviewed. Strategies toward overcoming systemic adverse events and the establishment of a suitable therapeutic margin for clinical studies are discussed. EXPERT OPINION: Preclinically, SCD-inhibition leads to reductions in body-weight gain, improvements in glucose clearance and improved liver-lipid profile. However, chronic SCD inhibition in skin and eye-lubricating glands results in undesirable adverse events. Several strategies to overcome these findings have been described, including alternative administration routes for acne or oncology applications, use of potent and rapidly cleared compounds and SCD-inhibitors with a liver-targeted tissue distribution profile. The attainment of sufficient therapeutic margin and robust efficacy for therapeutic applications in humans remains a major frontier for SCD-inhibitors.
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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 | 0.001 | 0.001 |
| Meta-epidemiology (narrow) | 0.001 | 0.000 |
| Meta-epidemiology (broad) | 0.001 | 0.001 |
| Bibliometrics | 0.004 | 0.003 |
| Science and technology studies | 0.000 | 0.000 |
| Scholarly communication | 0.001 | 0.001 |
| Open science | 0.001 | 0.001 |
| Research integrity | 0.001 | 0.002 |
| Insufficient payload (model declined to judge) | 0.009 | 0.005 |
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".