Shipston M J, Kelly J S, Antoni F A
Department of Pharmacology, University of Edinburgh, Edinburgh, Scotland, United Kingdom.
J Biol Chem. 1996 Apr 19;271(16):9197-200. doi: 10.1074/jbc.271.16.9197.
Adrenal corticosteroids have well known and profound effects on neurons and neuroendocrine cells, but the underlying cellular mechanisms are poorly understood. The present study analyzed membrane currents and ACTH release in AtT20 mouse pituitary corticotrope tumor cells. Patch-clamp analysis revealed a significant and selective inhibition of calcium-activated (BK-type) potassium channels upon activation of protein kinase A by corticotropin-releasing factor or 8-chlorophenylthio-cAMP. The synthetic glucocorticoid dexamethasone had no effect on potassium currents evoked by depolarization but prevented the inhibitory effect of protein kinase A activators. The action of dexamethasone had the hallmarks of protein induction, i.e. a lag time and sensitivity to inhibitors of DNA transcription and mRNA translation. In parallel, the specific BK channel blocker iberiotoxin abolished early glucocorticoid inhibition of corticotropin-releasing factor-stimulated ACTH secretion. In summary, the present data show that glucocorticoid-induced proteins render BK-type channels resistant to inhibition by protein kinase A and that this action of the steroid is pivotal for its early inhibitory effect on the secretion of ACTH.
肾上腺皮质类固醇对神经元和神经内分泌细胞具有众所周知的深远影响,但其潜在的细胞机制却知之甚少。本研究分析了AtT20小鼠垂体促肾上腺皮质激素瘤细胞中的膜电流和促肾上腺皮质激素(ACTH)释放情况。膜片钳分析显示,促肾上腺皮质激素释放因子或8-氯苯硫基-cAMP激活蛋白激酶A后,钙激活(BK型)钾通道受到显著且选择性的抑制。合成糖皮质激素地塞米松对去极化诱发的钾电流没有影响,但可阻止蛋白激酶A激活剂的抑制作用。地塞米松的作用具有蛋白质诱导的特征,即有延迟时间且对DNA转录和mRNA翻译抑制剂敏感。同时,特异性BK通道阻滞剂iberiotoxin消除了糖皮质激素对促肾上腺皮质激素释放因子刺激的ACTH分泌的早期抑制作用。总之,目前的数据表明,糖皮质激素诱导的蛋白质使BK型通道对蛋白激酶A的抑制产生抗性,并且这种类固醇的作用对其对ACTH分泌的早期抑制作用至关重要。