Piezo Channels
Piezo channels are mechanosensitive ion channels that mediate touch, hearing, proprioception, airway stretch sensation and blood pressure regulation. Piezo channel activation allows cation influx into cells resulting in membrane depolarization and activation of Ca2+-dependent signaling pathways.
Piezo Channel Modulators |
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|---|---|
| Cat. No. | Product Name / Activity |
| 6568 | Dooku 1 |
| Reversibly blocks Yoda1 activity; does not affect constitutive Piezo1 activity | |
Piezo Channel Inhibitors |
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| Cat. No. | Product Name / Activity |
| 4912 | GsMTx4 |
| Inhibits Piezo1 channels; also TRPC1 and TRPC6 blocker | |
| 7170 | D-GsMTx4 |
| Piezo2 and TRPC1/6 inhibitor; resistant to proteolytic digestion | |
Piezo Channel Activators |
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| Cat. No. | Product Name / Activity |
| 6614 | Jedi2 |
| Piezo1 channel activator | |
| 5586 | Yoda 1 |
| Piezo1 channel activator | |
| 8051 | Yoda 2 |
| Piezo1 channel activator | |
Other |
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| Cat. No. | Product Name / Activity |
| 6545 | OB-1 |
| Stomatin-like protein-3 (STOML3) oligomerization inhibitor | |
The Piezo proteins comprise an evolutionarily conserved family of proteins that have no apparent sequence homology with other known ion channels. There are two Piezo genes, PIEZO1 and PIEZO2, encoding large transmembrane proteins of over 2500 amino acids. Piezo1 proteins assemble as trimeric complexes having at least 42 transmembrane segments and forming a central pore with three peripheral "wings". The C-terminal regions (residues 2189 - 2549) of the three assembled proteins form the central ion-conducting pore, which bears structural similarity to the pore of other trimeric ion channels (ASIC1 and P2X4), while the N-terminal non-pore containing regions (residues 1 - 2190) serve as the mechanotransduction modules. The peripheral regions, or wings, comprise extracellular "blade" domains, intracellular "beam"-like structures that anchor the blades to the pore, and "anchor" domains. The blade domains are highly flexible and it is thought that the ion channel is activated as a result of the peripheral regions acting as force sensors and transducers.
Piezo1 is involved in shear-stress sensing in blood vessels and is important in the development and function of the circulatory system. It is expressed in red blood cells and has a role in blood cell homeostasis. It is also implicated as a sensor of mechanical forces in endothelial, urothelial and epithelial cells. Piezo2 is expressed in sensory neurons and auditory hair cells and is key in touch sensation and proprioception, respiratory function and hearing.