Voltage‐Gated Ion Channels: Structure, Pharmacology and Photopharmacology

Abstract: Voltage‐gated ion channels are transmembrane proteins responsible for the generation and propagation of action potentials in excitable cells. Over the last decade, advancements have enabled the elucidation of crystal structures of ion channels. This progress in structural understanding, particularly in identifying the binding sites of local anesthetics, opens avenues for the design of novel compounds capable of modulating ion conduction. However, many traditional drugs lack selectivity and come with adverse side effects. The emergence of photopharmacology has provided an orthogonal way of controlling the activity of compounds, enabling the regulation of ion conduction with light. In this review, we explore the central pore region of voltage‐gated sodium and potassium channels, providing insights from both structural and pharmacological perspectives. We discuss the different binding modes of synthetic compounds that can physically occlude the pore and, therefore, block ion conduction. Moreover, we examine recent advances in the photopharmacology of voltage‐gated ion channels, introducing molecular approaches aimed at controlling their activity by using photosensitive drugs.

Standort
Deutsche Nationalbibliothek Frankfurt am Main
Umfang
Online-Ressource
Sprache
Englisch

Erschienen in
Voltage‐Gated Ion Channels: Structure, Pharmacology and Photopharmacology ; day:17 ; month:07 ; year:2024 ; extent:16
ChemPhysChem ; (17.07.2024) (gesamt 16)

Urheber
Palmisano, Vito F.
Anguita‐Ortiz, Nuria
Faraji, Shirin
Nogueira, Juan J.

DOI
10.1002/cphc.202400162
URN
urn:nbn:de:101:1-2407181421589.326669440600
Rechteinformation
Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
Letzte Aktualisierung
14.08.2025, 10:43 MESZ

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Beteiligte

  • Palmisano, Vito F.
  • Anguita‐Ortiz, Nuria
  • Faraji, Shirin
  • Nogueira, Juan J.

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