Wilkins Benjamin J, Dai Yan-Shan, Bueno Orlando F, Parsons Stephanie A, Xu Jian, Plank David M, Jones Fred, Kimball Thomas R, Molkentin Jeffery D
Division of Molecular Cardiovascular Biology, Department of Pediatrics, Children's Hospital Medical Center, 3333 Burnet Ave, Cincinnati, Ohio 45229-3039, USA.
Circ Res. 2004 Jan 9;94(1):110-8. doi: 10.1161/01.RES.0000109415.17511.18. Epub 2003 Dec 1.
Calcineurin (PP2B) is a calcium/calmodulin-activated, serine-threonine phosphatase that transmits signals to the nucleus through the dephosphorylation and translocation of nuclear factor of activated T cell (NFAT) transcription factors. Whereas calcineurin-NFAT signaling has been implicated in regulating the hypertrophic growth of the myocardium, considerable controversy persists as to its role in maintaining versus initiating hypertrophy, its role in pathological versus physiological hypertrophy, and its role in heart failure. To address these issues, NFAT-luciferase reporter transgenic mice were generated and characterized. These mice showed robust and calcineurin-specific activation in the heart that was inhibited with cyclosporin A. In the adult heart, NFAT-luciferase activity was upregulated in a delayed, but sustained manner throughout eight weeks of pathological cardiac hypertrophy induced by pressure-overload, or more dramatically following myocardial infarction-induced heart failure. In contrast, physiological hypertrophy as produced in two separate models of exercise training failed to show significant calcineurin-NFAT coupling in the heart at multiple time points, despite measurable increases in heart to body weight ratios. Moreover, stimulation of hypertrophy with growth hormone-insulin-like growth factor-1 (GH-IGF-1) failed to activate calcineurin-NFAT signaling in the heart or in culture, despite hypertrophy, activation of Akt, and activation of p70 S6K. Calcineurin Abeta gene-targeted mice also showed a normal hypertrophic response after GH-IGF-1 infusion. Lastly, exercise- or GH-IGF-1-induced cardiac growth failed to show induction of hypertrophic marker gene expression compared with pressure-overloaded animals. Although a direct cause-and-effect relationship between NFAT-luciferase activity and pathological hypertrophy was not proven here, our results support the hypothesis that separable signaling pathways regulate pathological versus physiological hypertrophic growth of the myocardium, with calcineurin-NFAT potentially serving a regulatory role that is more specialized for maladaptive hypertrophy and heart failure.
钙调神经磷酸酶(PP2B)是一种钙/钙调蛋白激活的丝氨酸-苏氨酸磷酸酶,它通过活化T细胞核因子(NFAT)转录因子的去磷酸化和易位将信号传递至细胞核。尽管钙调神经磷酸酶-NFAT信号通路与心肌肥厚生长的调节有关,但其在维持与启动肥厚、病理肥厚与生理肥厚以及心力衰竭中的作用仍存在相当大的争议。为了解决这些问题,构建并鉴定了NFAT-荧光素酶报告基因转基因小鼠。这些小鼠心脏中呈现出强大且钙调神经磷酸酶特异性的激活,该激活可被环孢素A抑制。在成年心脏中,压力超负荷诱导的病理性心脏肥厚持续8周期间,NFAT-荧光素酶活性以延迟但持续的方式上调,在心肌梗死诱导的心力衰竭后上调更为显著。相比之下,在两个不同的运动训练模型中产生的生理肥厚,尽管心脏与体重比有可测量的增加,但在多个时间点心脏中均未显示出显著的钙调神经磷酸酶-NFAT偶联。此外,生长激素-胰岛素样生长因子-1(GH-IGF-1)刺激肥厚,尽管出现了肥厚、Akt激活和p70 S6K激活,但在心脏或培养物中未能激活钙调神经磷酸酶-NFAT信号通路。钙调神经磷酸酶β基因靶向小鼠在输注GH-IGF-1后也表现出正常的肥厚反应。最后,与压力超负荷动物相比,运动或GH-IGF-1诱导的心脏生长未能显示肥厚标志物基因表达的诱导。尽管此处未证明NFAT-荧光素酶活性与病理性肥厚之间存在直接的因果关系,但我们的结果支持以下假设:可分离的信号通路调节心肌的病理性与生理性肥厚生长,钙调神经磷酸酶-NFAT可能发挥更专门针对适应性不良肥厚和心力衰竭的调节作用。