Protein kinase C modulation of recombinant ATP‐sensitive K<sup>+</sup> channels composed of Kir6.1 and/or Kir6.2 expressed with SUR2B
Bibliographic record
Abstract
The molecular identity of smooth muscle ATP-sensitive K(+) channels (K(ATP)) is not established with certainty. Patch clamp methods were employed to determine if recombinant K(ATP) channels composed of Kir6.1 and SUR2B subunits expressed by human embryonic kidney (HEK293) cells share an identical modulation by protein kinase C (PKC) with the vascular K(NDP) subtype of K(ATP) channel. The open probability of Kir6.1/SUR2B channels was determined before and after sequential exposure to pinacidil (50 microM) and the combination of pinacidil and phorbol 12,13-dibutyrate (PdBu; 50 nM). Treatment with PdBu caused a decline in channel activity, but this was not seen with an inactive phorbol ester, 4 alpha-phorbol 12,13-didecanoate (PdDe; 50 nM). Angiotensin II (0.1 microM) induced a similar inhibition of Kir6.1/SUR2B channels in cells expressing angiotensin AT(1) receptors. The effects of PdBu and angiotensin II were blocked by the PKC inhibitor, chelerythrine (3 microM). Purified PKC inhibited Kir6.1/SUR2B activity (in 0.5 mM ATP/ 0.5 mM ADP), and the inhibition was blocked by a specific peptide inhibitor of PKC, PKC(19-31). In contrast, PdBu increased the activity of recombinant K(ATP) channels composed of Kir6.2 and SUR2B, or the combination of Kir6.1, Kir6.2 and SUR2B subunits. The results indicate that the modulation by PKC of Kir6.1/SUR2B, but not Kir6.2/SUR2B or Kir6.1-Kir6.2/SUR2B channel gating mimics that of native vascular K(NDP) channels. Physiological inhibition of vascular K(ATP) current by vasoconstrictors which utilize intracellular signalling cascades involving PKC is concluded to involve the modulation of K(NDP) channel complexes composed of four Kir6.1 and their associated SUR2B subunits.
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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".