The DOI matches its Crossref record; 1 of the 1 references it cites were found in a registry or an index.
Chemical activation of the mechanotransduction channel Piezo1
Open accessAbstract
Piezo ion channels are activated by various types of mechanical stimuli and function as biological pressure sensors in both vertebrates and invertebrates. To date, mechanical stimuli are the only means to activate Piezo ion channels and whether other modes of activation exist is not known. In this study, we screened ∼3.25 million compounds using a cell-based fluorescence assay and identified a synthetic small molecule we termed Yoda1 that acts as an agonist for both human and mouse Piezo1. Functional studies in cells revealed that Yoda1 affects the sensitivity and the inactivation kinetics of mechanically induced responses. Characterization of Yoda1 in artificial droplet lipid bilayers showed that Yoda1 activates purified Piezo1 channels in the absence of other cellular components. Our studies demonstrate that Piezo1 is amenable to chemical activation and raise the possibility that endogenous Piezo1 agonists might exist. Yoda1 will serve as a key tool compound to study Piezo1 regulation and function.
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Citations
Cites
The Mechanosensitive Ion Channel Piezo1 Is Inhibited by the Peptide GsMTx4
Bae, C., Sachs, F., & Gottlieb, P. A. (2011) · Biochemistry · doi:10.1021/bi200770q · Cited by 566
Cited by
Mechanically Activated Ion Channels
Ranade, S. S., Syeda, R., & Patapoutian, A. (2015) · Neuron · doi:10.1016/j.neuron.2015.08.032 · Cited by 652
Self-citationMechanically activated ion channel Piezo1 modulates macrophage polarization and stiffness sensing
Atcha, H., Jairaman, A., Holt, J. R., Meli, V. S., Nagalla, R. R., Veerasubramanian, P. K., Brumm, K. T., Lim, H. E., Othy, S., Cahalan, M. D., et al. (2021) · Nature Communications · doi:10.1038/s41467-021-23482-5 · Cited by 644
Structure and mechanogating mechanism of the Piezo1 channel
Zhao, Q., Zhou, H., Chi, S., Wang, Y., Wang, J., Geng, J., Wu, K., Liu, W., Zhang, T., Dong, M.-Q., et al. (2018) · Nature · doi:10.1038/nature25743 · Cited by 628
Endothelial cation channel PIEZO1 controls blood pressure by mediating flow-induced ATP release
Wang, S., Chennupati, R., Kaur, H., Iring, A., Wettschureck, N., & Offermanns, S. (2016) · Journal of Clinical Investigation · doi:10.1172/jci87343 · Cited by 616
Piezos thrive under pressure: mechanically activated ion channels in health and disease
Murthy, S. E., Dubin, A. E., & Patapoutian, A. (2017) · Nature Reviews Molecular Cell Biology · doi:10.1038/nrm.2017.92 · Cited by 582
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Metadata
- Authors
- Syeda, R., Xu, J., Dubin, A. E., Coste, B., Mathur, J., Huynh, T., Matzen, J., Lao, J., Tully, D. C., Engels, I. H., Petrassi, H. M., Schumacher, A. M., Montal, M., Bandell, M., & Patapoutian, A.
- Venue
- eLife
- Publisher
- eLife Sciences Publications, Ltd
- Published
- 2015-05-22
- Volume
- 4
- ISSN
- 2050-084X (ISSN-L)
- OpenAlex
- W1928745964
- Cited by
- 737
- References
- 1
- FWCI
- 14.66
- Type
- journal article
- Language
- en
- Open access
- gold
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- Syeda, R., Xu, J., Dubin, A. E., Coste, B., Mathur, J., Huynh, T., Matzen, J., Lao, J., Tully, D. C., Engels, I. H., Petrassi, H. M., Schumacher, A. M., Montal, M., Bandell, M., & Patapoutian, A. (2015). Chemical activation of the mechanotransduction channel Piezo1. eLife. https://doi.org/10.7554/elife.07369
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