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

Author:

Van Nhung Thi Hong12ORCID,Kim Woo Kyung23ORCID,Nam Joo Hyun12ORCID

Affiliation:

1. Department of Physiology, Dongguk University College of Medicine, Gyeongju 38066, Republic of Korea

2. Channelopathy Research Center (CRC), Dongguk University College of Medicine, Goyang 10326, Republic of Korea

3. Department of Internal Medicine, Graduate School of Medicine, Dongguk University, Goyang 10326, Republic of Korea

Abstract

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.

Funder

Korean government

Dongguk University Research Fund

Publisher

MDPI AG

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