Evaluation of Neuroprotective and Adjuvant Activities of Diketopiperazine‐Based Peptidomimetics
Bibliographic record
Abstract
Abstract Oral delivery of peptide pharmaceuticals has long been a fundamental challenge in drug development. A new chemical platform has been developed based on branched 2,5‐diketopiperazines for creating orally active peptidomimetics. The platform includes a diketopiperazine bio‐carrier with “built‐in” functionally active peptide fragments or molecules coupled via linkers, transforming it into an orally available compound displaying the same type of activity. Based on this approach, we prepared several compounds that exhibit hemostimulating, hemosuppressing, and adjuvant activity. In this work, we screened the activity of substituted piperazine‐2,5‐dione derivatives in two experimental models: human neuroblastoma MC‐65 cells and as an adjuvant in response to ovalbumin invasion. As a result, some original cyclopeptide derivatives have demonstrated neuroprotective and adjuvant activity. The maximum neuroprotective activity was shown by cyclo‐[Glu(Ile)Glu(Trp)] and cyclo‐[AlaGlu(Trp)]; branched cyclopeptides containing a disaccharide component cyclo‐[L–Lys(N‐acetyl‐Glucosamine‐N‐acetyl‐muramyl)‐L‐Glu(L‐Trp‐OH)] and palmitic acid cyclo‐[L–Lys (Palmitoyl)‐L‐Glu(L‐Trp‐OH)] showed the highest adjuvant activity.
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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 | 0.000 |
| Insufficient payload (model declined to judge) | 0.001 | 0.000 |
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.
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".