Ontology highlight
ABSTRACT:
SUBMITTER: Liu C
PROVIDER: S-EPMC8244166 | biostudies-literature | 2021 Jan
REPOSITORIES: biostudies-literature
Liu Chang C Reese Rebecca R Vu Simon S Rougé Lionel L Shields Shannon D SD Kakiuchi-Kiyota Satoko S Chen Huifen H Johnson Kevin K Shi Yu Patrick YP Chernov-Rogan Tania T Greiner Demi Maria Zabala DMZ Kohli Pawan Bir PB Hackos David D Brillantes Bobby B Tam Christine C Li Tianbo T Wang Jianyong J Safina Brian B Magnuson Steve S Volgraf Matthew M Payandeh Jian J Zheng Jie J Rohou Alexis A Chen Jun J
Neuron 20201104 2
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 coval ...[more]