TRPA1 channel structural pharmacology!
TRPA1 is activated by a wide spectrum of covalent, noncovalent, natural, and synthetic compounds.
Many TRPA1 antagonists have been identified, and several compounds have been tested in human clinical trials with mixed outcomes.
Ten distinct ligand-binding sites have been revealed, spanning intracellular, transmembrane, and extracellular domains.
The unique ligand diversity and druggable sites underscore TRPA1’s broad physiological functions and therapeutic potential.
TRPA1 may serve as a powerful system for dissecting channel–ligand interactions and advancing structure-guided drug design.
https://www.cell.com/trends/pharmacological-sciences/fulltext/S0165-6147(26)00142-2
