The Mechanosensitive Ion Channel Piezo1 Is Inhibited by the Peptide GsMTx4
Open accessAbstract
Cells can respond to mechanical stress by gating mechanosensitive ion channels (MSCs). The cloning of Piezo1, a eukaryotic cation selective MSC, defines a new system for studying mechanical transduction at the cellular level. Because Piezo1 has electrophysiological properties similar to those of endogenous cationic MSCs that are selectively inhibited by the peptide GsMTx4, we tested whether the peptide targets Piezo1 activity. Extracellular GsMTx4 at micromolar concentrations reversibly inhibited ∼80% of the mechanically induced current of outside-out patches from transfected HEK293 cells. The inhibition was voltage insensitive, and as seen with endogenous MSCs, the mirror image d enantiomer inhibited like the l. The rate constants for binding and unbinding based on Piezo1 current kinetics provided association and dissociation rates of 7.0 × 10(5) M(-1) s(-1) and 0.11 s(-1), respectively, and a K(D) of ∼155 nM, similar to values previously reported for endogenous MSCs. Consistent with predicted gating modifier behavior, GsMTx4 produced an ∼30 mmHg rightward shift in the pressure-gating curve and was active on closed channels. In contrast, streptomycin, a nonspecific inhibitor of cationic MSCs, showed the use-dependent inhibition characteristic of open channel block. The peptide did not block currents of the mechanical channel TREK-1 on outside-out patches. Whole-cell Piezo1 currents were also reversibly inhibited by GsMTx4, and although the off rate was nearly identical to that of outside-out patches, differences were observed for the on rate. The ability of GsMTx4 to target the mechanosensitivity of Piezo1 supports the use of this channel in high-throughput screens for pharmacological agents and diagnostic assays.
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Current Piezo1 modulators, such as GsMTx4, have been shown to block Piezo1-mediated currents in vitro.
“Current Piezo1 modulators, such as the peptide inhibitor GsMTx4, have been shown to block Piezo1-mediated currents in vitro.144”
From Mechanosensitive calcium ion channels Piezo1: A therapeutic target in liver disease (2025) · cites this paper as [144]
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- Authors
- Bae, C., Sachs, F., & Gottlieb, P. A.
- Affiliations
- University at Buffalo, State University of New York (US)
- Corresponding author
- Sachs, Frederick
- Gottlieb, Philip A.
- Venue
- Biochemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2011-06-29
- Volume
- 50
- Issue
- 29
- Pages
- 6295-6300
- ISSN
- 0006-2960 (ISSN-L)
- 1520-4995
- PMC
- PMC3169095
- OpenAlex
- W1972071814
- Cited by
- 566
- References
- 32
- Citations by year
- 2026: 68 · 2025: 71 · 2024: 62 · 2023: 53 · 2022: 53 · 2021: 48 · 2020: 38 · 2019: 35 · 2018: 21 · 2017: 29 · 2016: 16 · 2015: 18 · 2014: 20 · 2013: 9 · 2012: 20
- FWCI
- 9.14
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- Biochemistry (publishedVersion)
- PubMed (publishedVersion)
- PubMed Central (acceptedVersion)
- Funders
- National Heart, Lung, and Blood Institute (R01HL054887)
- Topics
- Life Sciences › Neuroscience › Sensory Systems › Ion Channels and Receptors
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Ion channel regulation and function
- Health Sciences › Medicine › Physiology › Erythrocyte Function and Pathophysiology
- Keywords
- Piezo1, GsMTx4, mechanosensitive ion channels, cation channels, peptide inhibition, mechanical signal transduction, channel gating, open channel block, TREK-1, binding kinetics, dissociation rate constant
- MeSH terms
- Humans, Ion Channels, Kinetics, Peptides, Spider Venoms, Ion Channel Gating, Intercellular Signaling Peptides and Proteins, Mechanotransduction, Cellular, HEK293 Cells
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