机制(生物学)
离子通道
药理学
功能(生物学)
作用机理
神经科学
生物物理学
细胞内
医学
瞬时受体电位通道
受体
作者
Daniel Bakowski,Fraser Murray,Anant B. Parekh
出处
期刊:Annual Review of Pharmacology and Toxicology
[Annual Reviews]
日期:2021-01-07
卷期号:61 (1): 629-654
被引量:7
标识
DOI:10.1146/annurev-pharmtox-031620-105135
摘要
Calcium (Ca2+) release-activated Ca2+ (CRAC) channels are a major route for Ca2+ entry in eukaryotic cells. These channels are store operated, opening when the endoplasmic reticulum (ER) is depleted of Ca2+, and are composed of the ER Ca2+ sensor protein STIM and the pore-forming plasma membrane subunit Orai. Recent years have heralded major strides in our understanding of the structure, gating, and function of the channels. Loss-of-function and gain-of-function mutants combined with RNAi knockdown strategies have revealed important roles for the channel in numerous human diseases, making the channel a clinically relevant target. Drugs targeting the channels generally lack specificity or exhibit poor efficacy in animal models. However, the landscape is changing, and CRAC channel blockers are now entering clinical trials. Here, we describe the key molecular and biological features of CRAC channels, consider various diseases associated with aberrant channel activity, and discuss targeting of the channels from a therapeutic perspective.
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