Piezo-type mechanosensitive ion channel component 1 (PIEZO1) (PIEZO1)

Piezo-type mechanosensitive ion channel component 1 (PIEZO1) is a specialized transmembrane protein that acts as a non-selective cation channel, directly converting mechanical forces into electrochemical signals [UniProt; Nature, 2010]. It is a critical mediator of mechanotransduction, sensing stimuli such as shear stress in blood vessels and mechanical loading in bone [Nature, 2014; Nature, 2019]. Biologically, PIEZO1 is essential for vascular development, red blood cell volume homeostasis, and the maintenance of skeletal integrity [Blood, 2017; Nature, 2019]. Mutations in PIEZO1 are associated with several human diseases, including dehydrated hereditary stomatocytosis and lymphatic malformations [Blood, 2017; Nature Communications, 2015]. In oncology, PIEZO1 expression is often dysregulated, influencing tumor cell migration and stiffness-sensing [Nature, 2023]. While no PIEZO1-targeted therapies are currently FDA-approved, small molecule modulators like the agonist Yoda1 and the peptide inhibitor GsMTx4 are widely used in research to explore its therapeutic potential in cardiovascular and hematological conditions [eLife, 2015; Biochemistry, 2011].

Other names

FAM38AMembrane protein induced by beta-amyloidDehydrated hereditary stomatocytosis proteinMib

Agonism via chemical activation of the mechanosensitive gate (e.g., Yoda1) and Antagonism via pore blockade or stabilization of the closed state (e.g., GsMTx4) [eLife, 2015; Biochemistry, 2011].