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A Potent and Site-Selective Agonist of TRPA1

A Potent and Site-Selective Agonist of TRPA1

Junichiro Takaya, Kazuhiro Mio, Takuya Shiraishi, Tatsuki Kurokawa, Shinya Otsuka, Yasuo Mori, Motonari Uesugi

J Am Chem Soc. 2015 Dec 23;137(50):15859-64.

PMID: 26630251

Abstract:

TRPA1 is a member of the transient receptor potential (TRP) cation channel family that is expressed primarily on sensory neurons. This chemosensor is activated through covalent modification of multiple cysteine residues with a wide range of reactive compounds including allyl isothiocyanate (AITC), a spicy component of wasabi. The present study reports on potent and selective agonists of TRPA1, discovered through screening 1657 electrophilic molecules. In an effort to validate the mode of action of hit molecules, we noted a new TRPA1-selective agonist, JT010 (molecule 1), which opens the TRPA1 channel by covalently and site-selectively binding to Cys621 (EC50 = 0.65 nM). The results suggest that a single modification of Cys621 is sufficient to open the TRPA1 channel. The TRPA1-selective probe described herein might be useful for further mechanistic studies of TRPA1 activation.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP917562335	JT010		917562-33-5	Price

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