Challenges in the Therapeutic Targeting of KCa Channels: From Basic Physiology to Clinical Applications

Calcium-activated potassium (KCa) channels are ubiquitously expressed throughout the body and are able to regulate membrane potential and intracellular calcium concentrations, thereby playing key roles in cellular physiology and signal transmission. Consequently, it is unsurprising that KCa channels...

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Bibliographic Details
Published in:International journal of molecular sciences 2024-03, Vol.25 (5), p.2965
Main Authors: Van, Nhung Thi Hong, Kim, Woo Kyung, Nam, Joo Hyun
Format: Article
Language:English
Subjects:
Binding sites
BK channels
Calcium - metabolism
Cardiovascular System - metabolism
Cloning
Humans
IK channels
KCa channel modulators
KCa channels
Membrane Potentials
Permeability
Pharmaceutical Preparations
Physiology
Potassium
Potassium Channels, Calcium-Activated
Protons
Review
Sensors
SK channels
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Summary:Calcium-activated potassium (KCa) channels are ubiquitously expressed throughout the body and are able to regulate membrane potential and intracellular calcium concentrations, thereby playing key roles in cellular physiology and signal transmission. Consequently, it is unsurprising that KCa channels have been implicated in various diseases, making them potential targets for pharmaceutical interventions. Over the past two decades, numerous studies have been conducted to develop KCa channel-targeting drugs, including those for disorders of the central and peripheral nervous, cardiovascular, and urinary systems and for cancer. In this review, we synthesize recent findings regarding the structure and activating mechanisms of KCa channels. We also discuss the role of KCa channel modulators in therapeutic medicine. Finally, we identify the major reasons behind the delay in bringing these modulators to the pharmaceutical market and propose new strategies to promote their application.
ISSN:1422-0067
1661-6596
1422-0067
DOI:10.3390/ijms25052965