P2X receptors: dawn of the post-structure era.

P2X receptors: dawn of the post-structure era.
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DOI:
10.1016/j.tibs.2009.09.006
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发表时间:
2010-02
影响因子:
13.8
通讯作者:
Young, Mark T.
Young, Mark T.
中科院分区:
生物学1区
文献类型:
--
作者:
Young, Mark T.

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P2 X受体是由细胞外ATP门控的非选择性阳离子通道。它们在各种生理过程中发挥关键作用,如神经传递,疼痛感觉和对炎症的反应,使它们成为治疗炎性疼痛的有吸引力的药物靶标。斑马鱼P2X4.1的三维(3D)晶体结构的最近报告代表了我们对这些膜离子通道的理解的一个步骤变化,以前只有低分辨率的结构数据和间接结构-功能研究的推论。这篇评论的目的是将以前的工作放在新的3D结构的背景下,并总结了P2 X研究人员在进入后结构时代时面临的关键问题和挑战。
P2X receptors are non-selective cation channels gated by extracellular ATP. They play key roles in various physiological processes such as nerve transmission, pain sensation and the response to inflammation, making them attractive drug targets for the treatment of inflammatory pain. The recent report of the three-dimensional (3D) crystal structure of zebrafish P2X4.1 represents a step change in our understanding of these membrane ion channels, where previously only low-resolution structural data and inferences from indirect structure–function studies were available. The purpose of this review is to place previous work within the context of the new 3D structure, and to summarize the key questions and challenges which await P2X researchers as we move into the post-structure era.
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