Sandbox Reserved 1653: Difference between revisions

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.  

- [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.  

- [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 [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.