Analogues of the HIV-Tat peptide containing Nη-modified arginines as potent inhibitors of protein arginine N-methyltransferases
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Bibliographic record
Abstract
A series of Nη-modified peptides based upon the arginine-rich motif of the HIV-Tat peptide were synthesised and evaluated as substrates and inhibitors of three members of the protein arginine N-methyltransfferase (PRMT) family. PRMT1 and PRMT6 were shown to methylate each of the Tat-peptide analogues tested while PRMT4/CARM1 displayed a lower methylation activity against the same series of peptides. Kinetic assays further revealed that the Tat-peptide analogues also behave as potent substrate-inhibitors of PRMT1 and PRMT6 over specific enzyme concentration ranges. This work provides new insights into the methylating activity and inhibition of PRMTs when interacting with highly positively charged, multiple-arginine-containing peptides.
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Full frame distilled prediction
Teacher imitationNot calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.
Codex and Gemma teacher scores by category
| 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) | 0.000 | 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 it