Title |
Inhibitory effects of monoterpenes on human TRPA1 and the structural basis of their activity
|
---|---|
Published in |
The Journal of Physiological Sciences, October 2013
|
DOI | 10.1007/s12576-013-0289-0 |
Pubmed ID | |
Authors |
Masayuki Takaishi, Kunitoshi Uchida, Fumitaka Fujita, Makoto Tominaga |
Abstract |
TRPA1, one of the transient receptor potential channels, has been reported to be involved in nociception and inflammatory pain, suggesting that this molecule could be a promising target for the development of analgesic agents. We screened several monoterpene analogs of camphor, which is known to inhibit human (h) TRPA1, to identify more effective naturally occurring TRPA1 antagonists. Borneol, 2-methylisoborneol, and fenchyl alcohol exhibited higher inhibitory effects on hTRPA1 activity than either camphor or 1,8-cineole. Our results revealed further that the S873, T874, and Y812 residues of hTRPA1 were involved in the inhibitory effects, suggesting that the hydroxyl group in the six-membered ring of the inhibitors may be interacting with these amino acids. Further research on these identified TRPA1 antagonists could lead to new pain therapeutics. |
X Demographics
Geographical breakdown
Country | Count | As % |
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Japan | 1 | 50% |
Unknown | 1 | 50% |
Demographic breakdown
Type | Count | As % |
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Members of the public | 2 | 100% |
Mendeley readers
Geographical breakdown
Country | Count | As % |
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United Kingdom | 1 | 1% |
Unknown | 67 | 99% |
Demographic breakdown
Readers by professional status | Count | As % |
---|---|---|
Student > Ph. D. Student | 12 | 18% |
Student > Bachelor | 8 | 12% |
Researcher | 7 | 10% |
Other | 7 | 10% |
Student > Master | 7 | 10% |
Other | 15 | 22% |
Unknown | 12 | 18% |
Readers by discipline | Count | As % |
---|---|---|
Agricultural and Biological Sciences | 15 | 22% |
Medicine and Dentistry | 10 | 15% |
Biochemistry, Genetics and Molecular Biology | 9 | 13% |
Pharmacology, Toxicology and Pharmaceutical Science | 8 | 12% |
Chemistry | 6 | 9% |
Other | 3 | 4% |
Unknown | 17 | 25% |