药效团
化学
虚拟筛选
兴奋剂
瞬时受体电位通道
药物发现
生物活性
药理学
受体
生物化学
体外
医学
作者
Hiroaki Iwata,Naoto Kanda,Mitsugu Araki,Yukari Sagae,Koichi Masuda,Yasushi Okuno
标识
DOI:10.1016/j.bmcl.2020.127639
摘要
Transient receptor potential cation channel subfamily A member 1 (TRPA1), a member of the transient receptor potential family, detects a wide range of environmental stimuli, such as low temperature, abnormal pH, and reactive irritants. TRPA1 is of great interest as a target protein in fields related to pharmaceuticals and foods. In this study, a library of natural products was explored to identify TRPA1 activators by pharmacophore screening of known TRPA1 agonists and biological assays for agonist activity. The study identified six natural compounds as novel TRPA1 agonists. The discovery of these compounds may prove useful in elucidating the TRPA1 activation mechanism.
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