MAPPING THE LIGAND INTERACTION OF THE AT1 –RECEPTOR WITH PHOTOPROBES IN ALL POSITIONS OF ANGIOTENSIN II
Bibliographic record
Abstract
We have combined a photoaffinity labelling approach to study the molecular structure of the liganded human angiotensin II (AngII) type 1 receptor (hAT1). Systematic incorporation of the photoprobes p‐benzoyl‐L‐phenylalanine (Bpa) or p–[3–(trifluoromethyl)–3H–diazirin–3–yl]–L–phenylalanine (Tdf) into each of the eight positions of the AngII sequence was carried out. Since the constitutively active mutant [N111G]‐hAT1 (hAT1‐CAM) had a more permissive structure‐activity relationship, photoaffinity labelling studies were carried out on this CAM‐receptor. The AngII‐photoprobe analogues substituted in position 1, 2, 3 and 5 displayed AngII‐like properties on hAT1‐CAM. Analogues substituted in position 7 and 8 were shown to be low nM affinity neutral antagonists whereas analogues substituted in positions 4 and 6 had too low affinities. Receptor labelling experiments evidence localisation of the peptide N‐terminus in the extracellular space of the receptor through contact with most extracellular elements of hAT1 A single contact with ECL2 was found at position 3 of AngII. The middle sequence elements are still ill‐defined but the AngII C‐terminal is in close contact with the trans‐membrane bundle formed by TMD3, 5, 6 and 7, in accord with previous results (Clement, JBC. 2005; 280:27121). This study again confirms the extended ligand structure in the hAT1 receptor.
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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 | 0.001 | 0.001 |
| Insufficient payload (model declined to judge) | 0.001 | 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".