Limapichat Walrati, Dougherty Dennis A, Lester Henry A
Divisions of Chemistry and Chemical Engineering (W.L., D.A.D.) and Biology and Biological Engineering (H.A.L.), California Institute of Technology, Pasadena, California.
Divisions of Chemistry and Chemical Engineering (W.L., D.A.D.) and Biology and Biological Engineering (H.A.L.), California Institute of Technology, Pasadena, California
Mol Pharmacol. 2014 Sep;86(3):263-74. doi: 10.1124/mol.114.093179. Epub 2014 Jun 25.
P2X receptors and nicotinic acetylcholine receptors (nAChRs) display functional and physical interactions in many cell types and heterologous expression systems, but interactions between α6β4-containing (α6β4*) nAChRs and P2X2 receptors and/or P2X3 receptors have not been fully characterized. We measured several types of crosstalk in oocytes coexpressing α6β4 nAChRs and P2X2, P2X3, or P2X2/3 receptors. A novel form of crosstalk occurs between α6β4 nAChRs and P2X2 receptors. P2X2 receptors were forced into a prolonged desensitized state upon activation by ATP through a mechanism that does not depend on the intracellular C terminus of the P2X2 receptors. Coexpression of α6β4 nAChRs with P2X3 receptors shifts the ATP dose-response relation to the right, even in the absence of acetylcholine (ACh). Moreover, currents become nonadditive when ACh and ATP are coapplied, as previously reported for other Cys-loop receptors interacting with P2X receptors, and this crosstalk is dependent on the presence of the P2X3 C-terminal domain. P2X2 receptors also functionally interact with α6β4β3 but through a different mechanism from α6β4. The interaction with P2X3 receptors is less pronounced for the α6β4β3 nAChR than the α6β4 nAChR. We also measured a functional interaction between the α6β4 nAChRs and the heteromeric P2X2/3 receptor. Experiments with the nAChR channel blocker mecamylamine on P2X2-α6β4 oocytes point to the loss of P2X2 channel activity during the crosstalk, whereas the ion channel pores of the P2X receptors were fully functional and unaltered by the receptor interaction for P2X2-α6β4β3, P2X2/3-α6β4, and P2X2/3-α6β4β3. These results may be relevant to dorsal root ganglion cells and to other neurons that coexpress these receptor subunits.
P2X受体和烟碱型乙酰胆碱受体(nAChRs)在许多细胞类型和异源表达系统中表现出功能和物理相互作用,但含α6β4的(α6β4*)nAChRs与P2X2受体和/或P2X3受体之间的相互作用尚未得到充分表征。我们在共表达α6β4 nAChRs与P2X2、P2X3或P2X2/3受体的卵母细胞中测量了几种类型的串扰。α6β4 nAChRs与P2X2受体之间发生了一种新型串扰。P2X2受体在被ATP激活后会通过一种不依赖于P2X2受体细胞内C末端的机制被迫进入长时间脱敏状态。α6β4 nAChRs与P2X3受体共表达会使ATP剂量-反应关系向右移动,即使在没有乙酰胆碱(ACh)的情况下也是如此。此外,当同时施加ACh和ATP时,电流变得不可叠加,正如先前报道的其他与P2X受体相互作用的半胱氨酸环受体一样,并且这种串扰依赖于P2X3 C末端结构域的存在。P2X2受体也与α6β4β3在功能上相互作用,但通过与α6β4不同的机制。α6β4β3 nAChR与P2X3受体的相互作用不如α6β4 nAChR明显。我们还测量了α6β4 nAChRs与异源P2X2/3受体之间的功能相互作用。用nAChR通道阻滞剂美加明对P2X2-α6β4卵母细胞进行的实验表明,在串扰过程中P2X2通道活性丧失,而对于P2X2-α6β4β3、P2X2/3-α6β4和P2X2/3-α6β4β3,P2X受体的离子通道孔功能完全正常且未因受体相互作用而改变。这些结果可能与背根神经节细胞以及其他共表达这些受体亚基的神经元有关。