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Special Issue "Ion Channels as Therapeutic Target: Drug Design and Pharmacological Investigation 2.0"

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Biochemistry".

Deadline for manuscript submissions: 30 November 2023 | Viewed by 642

Special Issue Editors

Dipartimento NEUROFARBA, Università degli Studi di Firenze, Via U. Schiff, 6, 50019 Polo Scientifico, Sesto Fiorentino, Firenze, Italy
Interests: heterocyclic nitrogen compounds; pyrazolo condensed compounds; synthesis; GABAA receptor subtype; human neutrophil elastase inhibitors; medicinal chemistry
Special Issues, Collections and Topics in MDPI journals
Dipartimento di Scienze Farmaceutiche, Università degli Studi di Firenze, via Ugo Schiff 6, 50019 Sesto Fiorentino, Italy
Interests: medicinal chemistry; organic synthesis; heterocycles; GABAA subtype receptors; HNE inhibitors; FPR

Special Issue Information

Dear Colleagues,

This Special Issue is a continuation of our previous Special Issue “Ion Channels as Therapeutic Target: Drug Design and Pharmacological Investigation”.

The targeting of ion channels represents a strategy for the treatment of several pathologies since they are responsible for ion fluxes across membranes and contribute to maintaining cellular functions in central and peripheral tissues. The ion channels include two principal types of membrane proteins:

  1. The ligand-gated ion channels (LGICs), opened by neurotransmitters or ligands that bind the orthosteric or allosteric sites involved in the overall fast synaptic transmission in the nervous system;
  2. Voltage-gated ion channels, opened or closed by a change in the electrical gradient across the membrane.

Ion channels are very intriguing targets, and the development of new techniques elucidating the structures of these channels (e.g., cryo-EM) contributes to the design of new potential therapeutic agents for the treatment of neurological and neurodegenerative diseases, cancer, metabolic syndrome, and pain.

This Special Issue, titled ‘Ion Channels as Therapeutic Target: Drug Design and Pharmacological Investigation’, aims to collect contributions related to the drug design, molecular modeling, pharmacological investigation, and therapeutic applications of ion channel ligands.

Dr. Gabriella Guerrini
Dr. Maria P. Giovannoni
Guest Editors

Manuscript Submission Information

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Published Papers (1 paper)

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Research

Article
κO-SrVIA Conopeptide, a Novel Inhibitor Peptide for Two Members of the Human EAG Potassium Channel Family
Int. J. Mol. Sci. 2023, 24(14), 11513; https://doi.org/10.3390/ijms241411513 - 15 Jul 2023
Viewed by 514
Abstract
The first conotoxin affecting the voltage-gated potassium channels of the EAG family was identified and characterized from the venom of the vermivorous species Conus spurius from the Gulf of Mexico. This conopeptide, initially named Cs68 and later designated κO-SrVIA, is extremely hydrophobic and [...] Read more.
The first conotoxin affecting the voltage-gated potassium channels of the EAG family was identified and characterized from the venom of the vermivorous species Conus spurius from the Gulf of Mexico. This conopeptide, initially named Cs68 and later designated κO-SrVIA, is extremely hydrophobic and comprises 31 amino acid residues, including six Cysteines in the framework VI/VII, and a free C-terminus. It inhibits the currents mediated by two human EAG subtypes, Kv10.1 (IC50 = 1.88 ± 1.08 µM) and Kv11.1 (IC50 = 2.44 ± 1.06 µM), and also the human subtype Kv1.6 (IC50 = 3.6 ± 1.04 µM). Despite its clear effects on potassium channels, it shares a high sequence identity with δ-like-AtVIA and δ-TsVIA. Also, κO-SrVIA is the third conopeptide from the venom of C. spurius with effects on potassium channels, and the seventh conotoxin that blocks Kv1.6 channels. Full article
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