Related Experiment Video
Updated: Jul 28, 2025
07:26
Cell-based Calcium Assay for Medium to High Throughput Screening of TRP Channel Functions using FlexStation 3
Published on: August 17, 2011
21.2K
ORAI Calcium Channels: Regulation, Function, Pharmacology, and Therapeutic Targets
1Department of Laboratory Medicine, Division of Clinical Pharmacology, Karolinska Institute and Karolinska University Hospital, C1:68, 141 86 Stockholm, Sweden.
Pharmaceuticals (Basel, Switzerland)
|June 1, 2023
Summary
Store-operated calcium entry (SOCE) involves Orai and STIM proteins, crucial for cell function and implicated in diseases. Targeting these calcium channels offers therapeutic potential for various human disorders.
Area of Science:
- Cell Biology
- Physiology
- Pharmacology
Background:
- Intracellular calcium (Ca2+) levels regulate diverse cell functions.
- Store-operated calcium entry (SOCE) is mediated by Orai and STIM proteins.
- Dysregulation of SOCE is linked to numerous human diseases.
Purpose of the Study:
- To review current knowledge on Orai/STIM channels in human diseases.
- To highlight Orai/STIM channels as potential drug targets.
- To discuss pharmacological modulators of Orai/STIM channels.
Main Methods:
- Literature review of Orai/STIM channel function and disease association.
- Analysis of Orai/STIM channel involvement in cell signaling pathways.
- Exploration of pharmacological agents targeting Orai/STIM complexes.
Main Results:
- Orai/STIM channels are implicated in immunodeficiency, myopathy, cardiovascular disorders, cancers, and more.
- These channels interact with key signaling receptors.
- Pharmacological targeting of Orai/STIM channels is a promising therapeutic strategy.
Conclusions:
- Orai/STIM channels play a critical role in human health and disease.
- Developing selective small molecules to modulate Orai/STIM channels is essential for therapeutic intervention.
- Further research into Orai/STIM channel biology will advance treatments for various disorders.
Related Concept Videos
01:30Ligand-Gated Ion Channel Receptor: Gating Mechanism
2.3K
Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...
2.3K
01:26Voltage-gated Ion Channels
8.3K
Voltage-gated ion channels are transmembrane proteins that open and close in response to changes in the membrane potential. They are present on the membranes of all electrically excitable cells such as neurons, heart, and muscle cells.
Generally, all voltage-gated ion channels have a 'voltage-sensing domain' that spans the lipid bilayer. The charged residues in the sensor move in response to the membrane potential changes that open the channel allowing ions movement. There are several...
Generally, all voltage-gated ion channels have a 'voltage-sensing domain' that spans the lipid bilayer. The charged residues in the sensor move in response to the membrane potential changes that open the channel allowing ions movement. There are several...
8.3K
01:24Non-gated Ion Channels
6.9K
Ion channels are specialized proteins on the plasma membrane that allow charged ions to pass down their electrochemical gradient. Their main function is to maintain the membrane potential which is critical for cell viability. These channels are either gated or non-gated and can transport more than a thousand ions within milliseconds for the cellular event to occur.
Compared to the gated ion channels, the non-gated channels, also known as leakage or passive channels, have no gating mechanism....
Compared to the gated ion channels, the non-gated channels, also known as leakage or passive channels, have no gating mechanism....
6.9K
01:18Antihypertensive Drugs: Action of Calcium Channel Blockers
592
Calcium ions are essential to contract smooth muscle cells in blood vessels. They enter these cells through voltage-dependent calcium channels, specifically L-type calcium channels in the cell membrane. These L-type calcium channels are integral to the excitation-contraction coupling process in smooth muscle. When a stimulus is received by smooth muscle cells, their membrane depolarizes. This alteration in membrane potential instigates the opening of L-type calcium channels. As a result,...
592
01:27Feedback Regulation of Calcium Concentration
3.4K
Calcium is an essential signaling molecule required for various cellular functions. Calcium pumps and ion channels on cell and organellar membranes, such as those on the endoplasmic reticulum (ER), regulate calcium concentrations inside the cell. They remain closed, keeping the cytosolic calcium levels low at a resting state.
Various transmembrane receptors, such as G protein-coupled receptors (GPCRs), elicit a response to extracellular signals by increasing cytosolic calcium. Activated GPCRs...
Various transmembrane receptors, such as G protein-coupled receptors (GPCRs), elicit a response to extracellular signals by increasing cytosolic calcium. Activated GPCRs...
3.4K
01:25Antianginal Drugs: Calcium Channel Blockers and Ranolazine
577
Angina pectoris, a primary symptom of ischemic heart disease, requires careful pharmacological interventions. In this context, calcium channel blockers (CCBs) and ranolazine have emerged as crucial pharmacotherapeutic agents, providing deep insights into the complexities of angina management.
CCBs, a diverse class that includes dihydropyridines (nifedipine) and diphenylalkylamines (verapamil and diltiazem), exert their effect by blocking calcium channels in cardiac and smooth muscle cells. This...
CCBs, a diverse class that includes dihydropyridines (nifedipine) and diphenylalkylamines (verapamil and diltiazem), exert their effect by blocking calcium channels in cardiac and smooth muscle cells. This...
577