Evidence map›Paper›PMID 26680001›Full record

ArticleThe Journal of biological chemistry2016

Mambalgin-1 Pain-relieving Peptide, Stepwise Solid-phase Synthesis, Crystal Structure, and Functional Domain for Acid-sensing Ion Channel 1a Inhibition.

Gilles Mourier, Miguel Salinas, Pascal Kessler, Enrico A Stura, Mathieu Leblanc, Livia Tepshi, Thomas Besson, Sylvie Diochot, Anne Baron, Dominique Douguet and 2 more

Open access · hybridAbstract read
In one paragraph

Article in The Journal of biological chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 33 papers.

0numbers the graph read from it
0cells of the map it votes in
33citing papers in PubMed
2.6field-weighted citation impact, top 10% 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

33 citing papers in PubMed, 66 citations in OpenAlex.

  1. Review
  2. Review
  3. Therapeutic Promise and Biotechnological Prospects ofInternational journal of molecular sciences · 2025
    Review
  4. Review
  5. Article
  6. Review
  7. Article
  8. Article
  9. Review
  10. Article
  11. Article
  12. Review
  13. Article
  14. Review
  15. Review
  16. Article
  17. Mambalgin-3 potentiates human acid-sensing ion channel 1b under mild to moderate acidosis: Implications as an analgesic lead.Proceedings of the National Academy of Sciences of the United States of America · 2021
    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

12 authors at 3 institutions in 1 country.

Gilles MourierFrom the Commissariat à l'Energie Atomique, iBiTecS, Service d'Ingénierie Moléculaire des Protéines, 91191 Gif-sur-Yvette.
Miguel Salinasthe CNRS, Institut de Pharmacologie Moléculaire et Cellulaire, the Université de Nice Sophia Antipolis, and the LabEx Ion Channel Science and Therapeutics, UMR 7275, 06560 Valbonne, France.
Pascal KesslerFrom the Commissariat à l'Energie Atomique, iBiTecS, Service d'Ingénierie Moléculaire des Protéines, 91191 Gif-sur-Yvette.
Enrico A SturaFrom the Commissariat à l'Energie Atomique, iBiTecS, Service d'Ingénierie Moléculaire des Protéines, 91191 Gif-sur-Yvette.
Mathieu LeblancFrom the Commissariat à l'Energie Atomique, iBiTecS, Service d'Ingénierie Moléculaire des Protéines, 91191 Gif-sur-Yvette.
Livia TepshiFrom the Commissariat à l'Energie Atomique, iBiTecS, Service d'Ingénierie Moléculaire des Protéines, 91191 Gif-sur-Yvette.
Thomas Bessonthe CNRS, Institut de Pharmacologie Moléculaire et Cellulaire, the Université de Nice Sophia Antipolis, and the LabEx Ion Channel Science and Therapeutics, UMR 7275, 06560 Valbonne, France.
Sylvie Diochotthe CNRS, Institut de Pharmacologie Moléculaire et Cellulaire, the Université de Nice Sophia Antipolis, and the LabEx Ion Channel Science and Therapeutics, UMR 7275, 06560 Valbonne, France.
Anne Baronthe CNRS, Institut de Pharmacologie Moléculaire et Cellulaire, the Université de Nice Sophia Antipolis, and the LabEx Ion Channel Science and Therapeutics, UMR 7275, 06560 Valbonne, France.
Dominique Douguetthe CNRS, Institut de Pharmacologie Moléculaire et Cellulaire, the Université de Nice Sophia Antipolis, and.
Eric Linguegliathe CNRS, Institut de Pharmacologie Moléculaire et Cellulaire, the Université de Nice Sophia Antipolis, and the LabEx Ion Channel Science and Therapeutics, UMR 7275, 06560 Valbonne, France lingueglia@ipmc.cnrs.fr.
Denis ServentFrom the Commissariat à l'Energie Atomique, iBiTecS, Service d'Ingénierie Moléculaire des Protéines, 91191 Gif-sur-Yvette, denis.servent@cea.fr.
Commissariat à l'Énergie Atomique et aux Énergies Alternatives · FRUniversité Côte d'Azur · FRInstitut de Pharmacologie Moléculaire et Cellulaire · FR

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Mambalgins are peptides isolated from mamba venom that specifically inhibit a set of acid-sensing ion channels (ASICs) to relieve pain. We show here the first full stepwise solid phase peptide synthesis of mambalgin-1 and confirm the biological activity of the synthetic toxin both in vitro and in vivo. We also report the determination of its three-dimensional crystal structure showing differences with previously described NMR structures. Finally, the functional domain by which the toxin inhibits ASIC1a channels was identified in its loop II and more precisely in the face containing Phe-27, Leu-32, and Leu-34 residues. Moreover, proximity between Leu-32 in mambalgin-1 and Phe-350 in rASIC1a was proposed from double mutant cycle analysis. These data provide information on the structure and on the pharmacophore for ASIC channel inhibition by mambalgins that could have therapeutic value against pain and probably other neurological disorders.

Indexed as

Elapid VenomsPeptidesAcid Sensing Ion ChannelsAnimalsNuclear Magnetic Resonance, BiomolecularOocytesProtein Structure, SecondaryProtein Structure, TertiaryRatsXenopus laevisAcid Sensing Ion ChannelsAsic1 protein, ratElapid Venomsmambalgin-1, Dendroaspis polylepisPeptidesacid sensing ion channel (ASIC)mambalginpainpeptide chemical synthesispeptide interactionsodium channelstructural modeltoxinX-ray crystallography

Identifiers

PMID26680001
PMCPMC4742732
OpenAlexW2208459503

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.