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Piezo1 and its inhibitors: Overview and perspectives. | LitMetric

Piezo1 and its inhibitors: Overview and perspectives.

Eur J Med Chem

Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, Freie Universität Berlin, Königin-Luise-Straße 2+4, Berlin, 14195, Germany. Electronic address:

Published: July 2024

AI Article Synopsis

  • The text highlights the significance of Piezo1, a cation channel involved in converting mechanical signals into cellular responses, making it a promising target for new therapies.* -
  • Various Piezo1 inhibitors have been identified, including toxins and natural compounds, which show potential in treating chronic diseases linked to Piezo1 misexpression, such as hypertension and cancer.* -
  • While there's promising research on Piezo1 inhibitors, the field is still in early stages, with ongoing opportunities for development and challenges to address.*

Article Abstract

The cation channel Piezo1, a crucial mechanotransducer found in various organs and tissues, has gained considerable attention as a therapeutic target in recent years. Following this trend, several Piezo1 inhibitors have been discovered and studied for potential pharmacological properties. This review provides an overview of the structural and functional importance of Piezo1, as well as discussing the biological activities of Piezo1 inhibitors based on their mechanism of action. The compounds addressed include the toxin GsMTx4, Aβ peptides, certain fatty acids, ruthenium red and gadolinium, Dooku1, as well as the natural products tubeimoside I, salvianolic acid B, jatrorrhzine, and escin. The findings revealed that misexpression of Piezo1 can be associated with a number of chronic diseases, including hypertension, cancer, and hemolytic anemia. Consequently, inhibiting Piezo1 and the subsequent calcium influx can have beneficial effects on various pathological processes, as shown by many in vitro and in vivo studies. However, the development of Piezo1 inhibitors is still in its beginnings, with many opportunities and challenges remaining to be explored.

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Source
http://dx.doi.org/10.1016/j.ejmech.2024.116502DOI Listing

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