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Comment
. 2021 Jan 20;109(2):194-196.
doi: 10.1016/j.neuron.2020.12.017.

Insights into the Irritating Mechanisms of TRPA1 Revealed by Cryo-EM

Michael Fine  1 , Xiaochun Li  2
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Insights into the Irritating Mechanisms of TRPA1 Revealed by Cryo-EM

Michael Fine et al. Neuron. .
Free article

Abstract

TRPA1 is a promising target for the development of novel treatments for chronic pain. In this issue of Neuron, Liu et al. (2021) report a novel non-covalent TRPA1-biased agonist, GNE551, revealing a unique binding pocket by cryo-EM and activation properties that pave a path toward new avenues in the treatment of chronic pain.

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  • A Non-covalent Ligand Reveals Biased Agonism of the TRPA1 Ion Channel.
    Liu C, Reese R, Vu S, Rougé L, Shields SD, Kakiuchi-Kiyota S, Chen H, Johnson K, Shi YP, Chernov-Rogan T, Greiner DMZ, Kohli PB, Hackos D, Brillantes B, Tam C, Li T, Wang J, Safina B, Magnuson S, Volgraf M, Payandeh J, Zheng J, Rohou A, Chen J. Liu C, et al. Neuron. 2021 Jan 20;109(2):273-284.e4. doi: 10.1016/j.neuron.2020.10.014. Epub 2020 Nov 4. Neuron. 2021. PMID: 33152265 Free PMC article.

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