Magoski Neil S
Department of Physiology, Queen's University, Kingston, Ontario K7L 3N6, Canada.
J Neurosci. 2004 Jul 28;24(30):6833-41. doi: 10.1523/JNEUROSCI.1694-04.2004.
Ion channel regulation by closely associated kinases or phosphatases has emerged as a key mechanism for orchestrating neuromodulation. An exemplary case is the nonselective cation channel that drives the afterdischarge in Aplysia bag cell neurons. Initial studies showed that this channel is modulated by both a closely associated PKC and a serine/threonine protein phosphatase (PP). In excised, inside-out patches, the addition of ATP (a phosphate source) increases open probability (P(O)) through PKC, and this is reversed by the PP. Previous work also reported that, in certain cases, ATP can decrease cation channel P(O). The present study characterizes and provides a mechanism for this decreased P(O) ATP response. The kinetic change for channels inhibited by ATP was identical to the previously reported effect of exogenously applied protein kinase A (PKA) (i.e., a lengthening of the third closed-state time constant). The decreased P(O) ATP response was blocked by the PKA inhibitor peptide PKA(6-22), and its reversal was prevented by the PP inhibitor microcystin-LR. Furthermore, PKA(6-22) did not alter the increased P(O) ATP response. This suggests that both PKA and a PP are closely associated with these cation channels, but PKA and PKC are not simultaneously targeted. After an afterdischarge, the bag cell neurons are refractory and fail to respond to subsequent stimulation. The association of PKA with the cation channel may contribute to this decrease in excitability. Altering the constituents of a regulatory complex, such as exchanging PKA for PKC, may represent a general mechanism to precisely control ion channel function and excitability.
由紧密相关的激酶或磷酸酶对离子通道进行调节,已成为协调神经调节的关键机制。一个典型的例子是驱动海兔袋状细胞神经元后放电的非选择性阳离子通道。最初的研究表明,该通道受紧密相关的蛋白激酶C(PKC)和丝氨酸/苏氨酸蛋白磷酸酶(PP)共同调节。在切除的内面向外膜片中,添加ATP(一种磷酸盐来源)可通过PKC增加开放概率(P(O)),而PP可使其逆转。先前的研究还报道,在某些情况下,ATP可降低阳离子通道的P(O)。本研究对这种P(O)的ATP反应降低进行了表征并提供了一种机制。受ATP抑制的通道的动力学变化与先前报道的外源性应用蛋白激酶A(PKA)的作用相同(即第三个关闭状态时间常数延长)。P(O)的ATP反应降低被PKA抑制剂肽PKA(6 - 22)阻断,其逆转被PP抑制剂微囊藻毒素-LR阻止。此外,PKA(6 - 22)并未改变P(O)的ATP反应增加。这表明PKA和PP都与这些阳离子通道紧密相关,但PKA和PKC并非同时作用于这些通道。在一次后放电后,袋状细胞神经元变得不应期,且对随后的刺激无反应。PKA与阳离子通道的结合可能导致了这种兴奋性的降低。改变调节复合物的组成成分,如将PKA换成PKC,可能是精确控制离子通道功能和兴奋性的一种普遍机制。