Cover Picture: Structure‐Based Organic Synthesis of Drug Prototypes: A Personal Odyssey (ChemMedChem 12/2006)
Bibliographic record
Abstract
The cover picture shows the cyanobacterial linear peptides dysinosin A (RH) and chlorodysinosin A (RCl), members of the aeruginosin family of cyanobacterial linear peptides. Their structures and absolute configurations were determined by total synthesis and X‐ray co‐crystallization with the enzyme thrombin. The presence of one chlorine atom in the D ‐leucine residue of chlorodysinosin A remarkably increases the inhibition potency against thrombin and Factor VIIa relative to dysinosin A. Molecular mechanics simulations starting from the bound conformations of dysinosin A and its chloro analogue suggest a more restricted sampling of conformations for the latter around the χ 1 dihedral angle. The chlorine atom in chlorodysinosin A may also contribute to lipophilicity, leading to a better fit in the hydrophobic S 3 pocket, as illustrated in the partial X‐ray co‐crystal structure. The background of the picture shows Lizard Island in North Queensland, Australia, where dysinosin A was isolated from the Dysideidae family of marine sponges. For details, see the Review by S. Hanessian on p. 1300 ff.
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How this classification was reachedexpand
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) | 0.001 | 0.001 |
| Meta-epidemiology (broad) | 0.001 | 0.001 |
| Bibliometrics | 0.000 | 0.000 |
| Science and technology studies | 0.000 | 0.000 |
| Scholarly communication | 0.000 | 0.000 |
| Open science | 0.001 | 0.000 |
| Research integrity | 0.001 | 0.001 |
| Insufficient payload (model declined to judge) | 0.006 | 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 teacher head, 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".