Piezo Channel Inhibitors

The Piezo proteins comprise an evolutionarily conserved family of proteins that have no apparent sequence homology with other known ion channels. There are two Piezo genes, PIEZO1 and PIEZO2, encoding large transmembrane proteins of over 2500 amino acids. Piezo1 proteins assemble as trimeric complexes having at least 42 transmembrane segments and forming a central pore with three peripheral "wings". The C-terminal regions (residues 2189 - 2549) of the three assembled proteins form ...