Sandbox Reserved 1653: Difference between revisions
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Piezo1 is a protein discovered recently. Therefore, its potential in medicine is in constant evolution. | Piezo1 is a protein discovered recently. Therefore, its potential in medicine is in constant evolution. | ||
Piezo1 can be used as diagnostic biomarkers because it detects different mechanical forces and triggers a specific response adapted to the changes in the environment. For instance, it is sensitive to shear stress which has a major role in cardiovascular physiology. | Piezo1 can be used as diagnostic [https://en.wikipedia.org/wiki/Biomarker biomarkers] because it detects different mechanical forces and triggers a specific response adapted to the changes in the environment. For instance, it is sensitive to shear stress which has a major role in [https://en.wikipedia.org/wiki/Cardiovascular_physiology cardiovascular physiology]. | ||
This mechanosensitive receptor is a candidate for therapeutic innovation more specifically in the case of cardiovascular and neurodegenerative diseases. | This mechanosensitive receptor is a candidate for therapeutic innovation more specifically in the case of cardiovascular and neurodegenerative diseases. | ||
These new therapies could be based on Piezo1 pharmacological modulators. Recently, several modulators have been found. | These new therapies could be based on Piezo1 pharmacological modulators. Recently, several modulators have been found. | ||
- Antagonists like peptide GsMTx4 prevent the induction of demyelination, playing therefore a neuroprotective role. This peptide is an inhibitor of Piezo1. | - [https://en.wikipedia.org/wiki/Receptor_antagonist Antagonists] like peptide GsMTx4 prevent the induction of [https://en.wikipedia.org/wiki/Demyelinating_disease demyelination], playing therefore a neuroprotective role. This peptide is an inhibitor of Piezo1. | ||
- Agonists like Yoda1 (a synthetic small molecule) enhance channels opening leading to demyelination and damaging the central nervous system. This molecule can activate the Piezo1 channel without mechanical stimulation. However, it can be useful to suppress the migration of transformed cells like fibroblasts. Jedi2 is another chemical activator of Piezo1, but it doesn’t act on the same site as Yoda1. | - [https://en.wikipedia.org/wiki/Agonist Agonists] like [https://en.wikipedia.org/wiki/Yoda1 Yoda1] (a synthetic small molecule) enhance channels opening leading to demyelination and damaging the central nervous system. This molecule can activate the Piezo1 channel without mechanical stimulation. However, it can be useful to suppress the migration of transformed cells like [https://en.wikipedia.org/wiki/Fibroblast fibroblasts]. [https://en.wikipedia.org/wiki/Jedi2 Jedi2] is another chemical activator of Piezo1, but it doesn’t act on the same site as Yoda1. | ||
- Tubeimoside 1 (TBMS1) is an inhibitor of Yoda1 allowing a decrease of the activity of Piezo 1 channels in endothelial cells. The mechanism is still unclear but according to studies, TBMS1 might be a competitive inhibitor, meaning that it fixes itself on the same binding site as Yoda1 and is specific to Piezo1 channels. | - Tubeimoside 1 (TBMS1) is an inhibitor of Yoda1 allowing a decrease of the activity of Piezo 1 channels in endothelial cells. The mechanism is still unclear but according to studies, TBMS1 might be a [https://en.wikipedia.org/wiki/Competitive_inhibition competitive inhibitor], meaning that it fixes itself on the same binding site as Yoda1 and is specific to Piezo1 channels. | ||
Discovering those modulators allows a better understanding of the mechanisms of Piezo1 channels and highlights its usefulness in the pharmacological field. | Discovering those modulators allows a better understanding of the mechanisms of Piezo1 channels and highlights its usefulness in the pharmacological field. | ||