- Liu, Chang;
- Reese, Rebecca;
- Vu, Simon;
- Rougé, Lionel;
- Shields, Shannon D;
- Kakiuchi-Kiyota, Satoko;
- Chen, Huifen;
- Johnson, Kevin;
- Shi, Yu Patrick;
- Chernov-Rogan, Tania;
- Greiner, Demi Maria Zabala;
- Kohli, Pawan Bir;
- Hackos, David;
- Brillantes, Bobby;
- Tam, Christine;
- Li, Tianbo;
- Wang, Jianyong;
- Safina, Brian;
- Magnuson, Steve;
- Volgraf, Matthew;
- Payandeh, Jian;
- Zheng, Jie;
- Rohou, Alexis;
- Chen, Jun
The TRPA1 ion channel is activated by electrophilic compounds through the covalent modification of intracellular cysteine residues. How non-covalent agonists activate the channel and whether covalent and non-covalent agonists elicit the same physiological responses are not understood. Here, we report the discovery of a non-covalent agonist, GNE551, and determine a cryo-EM structure of the TRPA1-GNE551 complex, revealing a distinct binding pocket and ligand-interaction mechanism. Unlike the covalent agonist allyl isothiocyanate, which elicits channel desensitization, tachyphylaxis, and transient pain, GNE551 activates TRPA1 into a distinct conducting state without desensitization and induces persistent pain. Furthermore, GNE551-evoked pain is relatively insensitive to antagonist treatment. Thus, we demonstrate the biased agonism of TRPA1, a finding that has important implications for the discovery of effective drugs tailored to different disease etiologies.