Piezo1 and its inhibitors: Overview and perspectives

Area of Science:

• Biophysics
• Pharmacology
• Cell Biology

Background:

• The cation channel Piezo1 is a critical mechanotransducer involved in cellular processes.
• Dysregulation of Piezo1 is linked to chronic diseases such as hypertension, cancer, and hemolytic anemia.
• Piezo1 inhibitors are emerging as potential therapeutic agents.

Purpose of the Study:

• To review the structural and functional significance of Piezo1.
• To discuss the biological activities of various Piezo1 inhibitors.
• To highlight the therapeutic potential of targeting Piezo1 in disease.

Main Methods:

• Literature review of Piezo1 structure, function, and inhibitors.
• Analysis of the mechanisms of action for different classes of Piezo1 inhibitors.
• Synthesis of findings from in vitro and in vivo studies on Piezo1 inhibition.

Main Results:

• Piezo1's role in mechanotransduction and its implication in diseases are detailed.
• Various Piezo1 inhibitors, including GsMTx4, Aβ peptides, fatty acids, ruthenium red, gadolinium, Dooku1, tubeimoside I, salvianolic acid B, jatrorrhzine, and escin, are discussed.
• Inhibition of Piezo1 and subsequent calcium influx demonstrates beneficial effects in multiple pathological models.

Conclusions:

• Targeting Piezo1 offers a promising therapeutic strategy for various chronic diseases.
• Further research and development are needed to overcome challenges in creating effective Piezo1 inhibitors.
• The field of Piezo1 inhibition presents significant opportunities for drug discovery.