Evidence map›Paper›PMID 11118199›Full record

ArticleThe EMBO journal2000

The molecular basis of the specificity of action of K(ATP) channel openers.

C Moreau, H Jacquet, A L Prost, N D'hahan, M Vivaudou

Open access · bronzeAbstract read
In one paragraph

Article in The EMBO journal, 2000. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 54 papers.

0numbers the graph read from it
0cells of the map it votes in
54citing papers in PubMed
7.9field-weighted citation impact, top 2% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

54 citing papers in PubMed, 138 citations in OpenAlex.

  1. Article
  2. Article
  3. KThe Journal of pharmacology and experimental therapeutics · 2023
    Article
  4. CL-705G: a novel chemical Kir6.2-specific KFrontiers in pharmacology · 2023
    Article
  5. iScience · 2022
    Article
  6. Article
  7. Article
  8. Review
  9. The Pharmacology of ATP-Sensitive KHandbook of experimental pharmacology · 2021
    Article
  10. Article
  11. Article
  12. Genetic Discovery of ATP-Sensitive KCirculation. Arrhythmia and electrophysiology · 2019
    Review
  13. 2,2-Dimethyl-3,4-dihydro-2MedChemComm · 2019
    Article
  14. Article
  15. Article
  16. KATP Channels in the Cardiovascular System.Physiological reviews · 2016
    Review
  17. Article
  18. Article
  19. Article
  20. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

5 authors at 1 institution in 1 country.

C MoreauCEA, DBMS, Biophysique Moléculaire et Cellulaire (UMR CNRS/UJF/CEA 5090), 17 Rue des Martyrs, 38054 Grenoble, France. vivaudou@cea.fr
H Jacquet
A L Prost
N D'hahan
M Vivaudou
Université Grenoble Alpes · FR

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

K(ATP) channels incorporate a regulatory subunit of the ATP-binding cassette (ABC) transporter family, the sulfonylurea receptor (SUR), which defines their pharmacology. The therapeutically important K(+) channel openers (e.g. pinacidil, cromakalim, nicorandil) act specifically on the SUR2 muscle isoforms but, except for diazoxide, remain ineffective on the SUR1 neuronal/pancreatic isoform. This SUR1/2 dichotomy underpinned a chimeric strategy designed to identify the structural determinants of opener action, which led to a minimal set of two residues within the last transmembrane helix of SUR. Transfer of either residue from SUR2A to SUR1 conferred opener sensitivity to SUR1, while the reverse operation abolished SUR2A sensitivity. It is therefore likely that these residues form part of the site of interaction of openers with the channel. Thus, openers would target a region that, in other ABC transporters, is known to be tightly involved with the binding of substrates and other ligands. This first glimpse of the site of action of pharmacological openers should permit rapid progress towards understanding the structural determinants of their affinity and specificity.

Indexed as

ATP-Binding Cassette TransportersPotassium Channels, Inwardly RectifyingAmino Acid SequenceAnimalsCell MembraneCricetinaeCromakalimDiazoxideIon Channel GatingMiceModels, MolecularMolecular Sequence DataMuscle, SkeletalMutagenesis, Site-DirectedNeuronsNicorandilAbcc8 protein, mouseAbcc8 protein, ratAbcc9 protein, mouseAbcc9 protein, ratATP-Binding Cassette TransportersCromakalimDiazoxideNicorandilPinacidilPotassium ChannelsPotassium Channels, Inwardly RectifyingProtein IsoformsReceptors, DrugRecombinant Fusion ProteinsSulfonylurea Receptors

Identifiers

PMID11118199
PMCPMC305901
OpenAlexW2007334529

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.