Calcium-Permeable Ion Channels as Targets in Pharmacotherapy

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Pharmacology".

Deadline for manuscript submissions: closed (31 December 2023) | Viewed by 2805

Special Issue Editor

Department of Laboratory Medicine, Division of Clinical Pharmacology, Karolinska Institute & Karolinska University Hospital, C1:68, 141 86 Stockholm, Sweden
Interests: calcium channels; TRPC channels; ion channels
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Ion channels are pore-forming proteins that are involved and play essential roles in very important physiological and pathological processes; hence, they serve as therapeutic drug targets. Calcium (Ca2+) ions are universal second messengers that regulate many fundamental cell activities and influence almost every component of cellular life. Ca2+ signaling governs both millisecond-scale cellular activities, such as muscular contraction, and slower functions lasting hours or days, such as cell migration and gene transcription.

Ca2+-permeable ion channels permit the influx or outflux of Ca2+ across the cell membrane and play a critical role in human physiology and pathology. Therefore, these channels have served as therapeutic drug targets or potential targets for various human diseases and disorders for a considerable time. This issue will focus on the Ca2+-permeable ion channels that are responsible for the influx of extracellular Ca2+, and these channels are the voltage-gated L- and T-type, TRP superfamily, ORAIs (1-3), Piezo (1, 2), and P2X receptors, which are ligand-gated ion channels.

This Special Issue aims to provide a comprehensive summary of our current knowledge of the structure, regulation, function, and pharmacology of Ca2+-permeable ion channels in human diseases and disorders as targets for therapeutic intervention.

Dr. Hussein N. Rubaiy
Guest Editor

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Keywords

  • ion channel
  • calcium ion
  • TRP channels
  • ORAI
  • P2X
  • drug target
  • therapeutic
  • diseases

Published Papers (1 paper)

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Review

22 pages, 1602 KiB  
Review
ORAI Calcium Channels: Regulation, Function, Pharmacology, and Therapeutic Targets
by Hussein N. Rubaiy
Pharmaceuticals 2023, 16(2), 162; https://doi.org/10.3390/ph16020162 - 22 Jan 2023
Cited by 4 | Viewed by 2415
Abstract
The changes in intracellular free calcium (Ca2+) levels are one of the most widely regulators of cell function; therefore, calcium as a universal intracellular mediator is involved in very important human diseases and disorders. In many cells, Ca2+ inflow is [...] Read more.
The changes in intracellular free calcium (Ca2+) levels are one of the most widely regulators of cell function; therefore, calcium as a universal intracellular mediator is involved in very important human diseases and disorders. In many cells, Ca2+ inflow is mediated by store-operated calcium channels, and it is recognized that the store-operated calcium entry (SOCE) is mediated by the two partners: the pore-forming proteins Orai (Orai1-3) and the calcium store sensor, stromal interaction molecule (STIM1-2). Importantly, the Orai/STIM channels are involved in crucial cell signalling processes such as growth factors, neurotransmitters, and cytokines via interaction with protein tyrosine kinase coupled receptors and G protein-coupled receptors. Therefore, in recent years, the issue of Orai/STIM channels as a drug target in human diseases has received considerable attention. This review summarizes and highlights our current knowledge of the Orai/STIM channels in human diseases and disorders, including immunodeficiency, myopathy, tubular aggregate, Stormorken syndrome, York platelet syndrome, cardiovascular and metabolic disorders, and cancers, as well as suggesting these channels as drug targets for pharmacological therapeutic intervention. Moreover, this work will also focus on the pharmacological modulators of Orai/STIM channel complexes. Together, our thoughtful of the biology and physiology of the Orai/STIM channels have grown remarkably during the past three decades, and the next important milestone in the field of store-operated calcium entry will be to identify potent and selective small molecules as a therapeutic agent with the purpose to target human diseases and disorders for patient benefit. Full article
(This article belongs to the Special Issue Calcium-Permeable Ion Channels as Targets in Pharmacotherapy)
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