Related Experiment Video
Updated: Jul 9, 2025
12:09
Yeast Luminometric and Xenopus Oocyte Electrophysiological Examinations of the Molecular Mechanosensitivity of TRPV4
Published on: December 31, 2013
10.2K
Targeting Ion Channel TRPM4
Barbara Preti1, Jean-Sébastien Rougier2, Irida Papapostolou2
1Institute if Biochemistry and Molecular Medicine, University of Bern.
Chimia
|December 9, 2023
Summary
Researchers identified novel small molecules that inhibit the TRPM4 ion channel. These TRPM4 inhibitors were used to explore the channel's role in heart disease, immune disorders, and cancer.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- The transient receptor potential melastatin 4 (TRPM4) ion channel is widely present in the body.
- TRPM4 dysfunction or mutations are associated with various diseases.
- Understanding TRPM4's role is crucial for developing new therapeutic strategies.
Purpose of the Study:
- To identify and characterize small molecule inhibitors of the TRPM4 ion channel.
- To investigate the involvement of TRPM4 in the pathophysiology of cardiac conditions, immune diseases, and cancer.
Main Methods:
- High-throughput screening to identify TRPM4 inhibitors.
- Biochemical assays to determine inhibitor potency (low µM range).
- Molecular biology techniques and functional assays to study TRPM4 in disease models.
Main Results:
- Identification of novel small molecules with low micromolar inhibitory activity against TRPM4.
- Demonstration of TRPM4's contribution to cardiac conditions, immune diseases, and cancer.
- Establishment of a toolkit for further TRPM4 research.
Conclusions:
- TRPM4 is a druggable target for various diseases.
- Novel TRPM4 inhibitors provide valuable tools for studying TRPM4-related pathophysiology.
- Targeting TRPM4 may offer therapeutic potential in cardiovascular, immunological, and oncological conditions.
Related Concept Videos
01:12Mechanically-gated Ion Channels
6.4K
Mechanically-gated ion channels are proteins found in eukaryotic and prokaryotic cell membranes that open in response to mechanical stress. Tension, compression, swelling, and shear stress can alter the conformation of the protein, opening a transmembrane channel that allows the passage of ions for signal transmission. In eukaryotes, mechanically-gated channels are distributed in several regions like the neurons, lungs, skin, bladder, and heart, where they play critical roles in numerous...
6.4K
01:24Non-gated Ion Channels
6.8K
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....
6.8K
01:21G-Protein Gated Ion Channels
4.6K
GPCRs are primarily responsible for our sense of smell, taste, and vision. The binding of a sensory stimulus activates GPCR to stimulate effector proteins, many of which are ion channels in the sensory organs. GPCRs modulate the opening and closing of the target ion channels either directly by binding them, or by releasing second messengers that activate these channels. As ions move across the membrane, the membrane potential is altered, which induces an appropriate response.
Sensory...
Sensory...
4.6K
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
01:19Ligand-gated Ion Channels
12.4K
Ligand-gated ion channels are transmembrane proteins with a channel for ions to pass through and a binding site for a ligand. The channel opens only when a ligand attaches to the binding site.
Three Subfamilies of Ligand-gated Ion Channels
Ligand-gated ion channels fall into three subfamilies. The 'Cys-loop' includes the nicotinic acetylcholine receptors, γ-aminobutyric acid (GABA), glycine, and 5-hydroxytryptamine receptors. The second one is the 'Pore-loop' channels that...
Three Subfamilies of Ligand-gated Ion Channels
Ligand-gated ion channels fall into three subfamilies. The 'Cys-loop' includes the nicotinic acetylcholine receptors, γ-aminobutyric acid (GABA), glycine, and 5-hydroxytryptamine receptors. The second one is the 'Pore-loop' channels that...
12.4K
01:43Thermosensation
30.4K
Peripheral thermosensation is the perception of external temperature. A change in temperature (on the surface of the skin and other tissues) is detected by a family of temperature-sensitive ion channels called Transient Receptor Potential, or TRP, receptors. These receptors are located on free nerve endings. Those detecting cold temperatures are closer to the surface of the skin than the nerve endings detecting warmth. These thermoTRP channels, while temperature selective, have relatively...
30.4K