P2X7受体：从低电导通道向高电导通道的转变——一种神秘现象？
The P2X7 receptor: shifting from a low- to a high-conductance channel - an enigmatic phenomenon?
作者信息
Alves Luiz Anastacio, de Melo Reis Ricardo Augusto, de Souza Cristina Alves Magalhães, de Freitas Monica Santos, Teixeira Pedro Celso Nogueira, Neto Moreira Ferreira Dinarte, Xavier Robson Faria
机构信息
Fundação Oswaldo Cruz, Instituto Oswaldo Cruz, Laboratório de Comunicação Celular, Av. Brasil 4365, 21045-900 Rio de Janeiro, Brazil.
Instituto de Biofísica Carlos Chagas Filho, Universidade Federal do Rio de Janeiro, Rio de Janeiro, Brazil.
出版信息
Biochim Biophys Acta. 2014 Oct;1838(10):2578-87. doi: 10.1016/j.bbamem.2014.05.015. Epub 2014 May 21.
The general structure of the P2X7 receptor (P2X7R) is similar to the structure of other P2X receptor family members, with the exception of its C terminus, which is the longest of this family. The P2X7R activates several intracellular signaling cascades, such as the calmodulin, mitogen-activated protein kinase and phospholipase D pathways. At low concentrations of ATP (micromolar range), P2X7R activation opens a cationic channel, similarly to other P2X receptors. However, in the presence of high concentrations of ATP (millimolar range), it opens a pathway that allows the passage of larger organic cations and anions. Here, we discuss both the structural characteristics of P2X7R related to its remarkable functions and the proposed mechanisms, including the dilation of the endogenous pore and the integration of another channel. In addition, we highlight the importance of P2X7R as a therapeutic target.
P2X7受体（P2X7R）的总体结构与其他P2X受体家族成员的结构相似，但其C末端除外，该C末端是该家族中最长的。P2X7R激活多种细胞内信号级联反应，如钙调蛋白、丝裂原活化蛋白激酶和磷脂酶D途径。在低浓度ATP（微摩尔范围）下，P2X7R的激活会打开一个阳离子通道，这与其他P2X受体类似。然而，在高浓度ATP（毫摩尔范围）存在的情况下，它会打开一条允许更大的有机阳离子和阴离子通过的通道。在此，我们讨论了与P2X7R显著功能相关的结构特征以及提出的机制，包括内源性孔道的扩张和另一个通道的整合。此外，我们强调了P2X7R作为治疗靶点的重要性。
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