Polymodal ligand sensitivity of TRPA1 and its modes of interactions.

Polymodal ligand sensitivity of TRPA1 and its modes of interactions.
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DOI:
10.1085/jgp.200810138
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发表时间:
2009-03
期刊:
The Journal of general physiology
影响因子:
--
通讯作者:
Hwang SW
Hwang SW
中科院分区:
其他
文献类型:
--
作者:
Bang S;Hwang SW

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近年来,对外周痛觉机制的理解取得了显著进展,部分原因是感觉神经元中瞬时受体电位(TRP)离子通道的发现。在这些离子通道中,TRPA 1亚型引起了人们的关注,因为它能够感知来自外部和内部环境的广泛损伤信号,这为离子通道的调节提供了一种新的范式。在这个角度来看,我们专注于TRPA1配体和辅因子,这是分组方面的反应性和结合方式。TRPA1的结合机制和可能的药理学意义也将被讨论,因为TRPA1在信号感知中的多模态性表明该通道可能是疼痛调节的有希望的靶点。
Understanding the mechanism of peripheral pain sensation has progressed remarkably in recent years, in part thanks to the discovery of transient receptor potential (TRP) ion channels in sensory neurons. Among these ion channels, the TRPA1 subtype is attracting attention because of its ability to sense a wide spectrum of damage signals from external and internal environments, which provides for a novel paradigm for the modulation of ion channels. In this Perspective, we focus on the TRPA1 ligands and cofactors, which are grouped in terms of their reactivity and binding fashions. The mechanism (s) of binding and possible pharmacological implications on TRPA1 will also be discussed because the polymodality of TRPA1 in signal sensing suggests that this channel may be a promising target for pain modulation.
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