Rababa'h Abeer, Singh Sonal, Suryavanshi Santosh V, Altarabsheh Salah Eldien, Deo Salil V, McConnell Bradley K
Department of Clinical Pharmacy, Jordan University of Science and Technology, Irbid 22110, Jordan.
Department of Pharmacological and Pharmaceutical Sciences, University of Houston, Texas Medical Center, Houston, TX 77204, USA.
Int J Mol Sci. 2014 Dec 24;16(1):218-29. doi: 10.3390/ijms16010218.
The Beta-adrenergic receptors (β-ARs) stimulation enhances contractility through protein kinase-A (PKA) substrate phosphorylation. This PKA signaling is conferred in part by PKA binding to A-kinase anchoring proteins (AKAPs). AKAPs coordinate multi-protein signaling networks that are targeted to specific intracellular locations, resulting in the localization of enzyme activity and transmitting intracellular actions of neurotransmitters and hormones to its target substrates. In particular, mAKAP (muscle-selective AKAP) has been shown to be present on the nuclear envelope of cardiomyocytes with various proteins including: PKA-regulatory subunit (RIIα), phosphodiesterase-4D3, protein phosphatase-2A, and ryanodine receptor (RyR2). Therefore, through the coordination of spatial-temporal signaling of proteins and enzymes, mAKAP controls cyclic-adenosine monophosphate (cAMP) levels very tightly and functions as a regulator of PKA-mediated substrate phosphorylation leading to changes in calcium availability and myofilament calcium sensitivity. The goal of this review is to elucidate the critical compartmentalization role of mAKAP in mediating PKA signaling and regulating cardiomyocyte hypertrophy by acting as a scaffolding protein. Based on our literature search and studying the structure-function relationship between AKAP scaffolding protein and its binding partners, we propose possible explanations for the mechanism by which mAKAP promotes cardiac hypertrophy.
β-肾上腺素能受体(β-ARs)的刺激通过蛋白激酶A(PKA)底物磷酸化增强收缩性。这种PKA信号传导部分是由PKA与A激酶锚定蛋白(AKAPs)结合介导的。AKAPs协调靶向特定细胞内位置的多蛋白信号网络,导致酶活性的定位,并将神经递质和激素的细胞内作用传递至其靶底物。特别地,肌肉选择性AKAP(mAKAP)已被证明存在于心肌细胞的核膜上,与多种蛋白质包括:PKA调节亚基(RIIα)、磷酸二酯酶-4D3、蛋白磷酸酶-2A和兰尼碱受体(RyR2)共存。因此,通过蛋白质和酶的时空信号协调,mAKAP非常严格地控制环磷酸腺苷(cAMP)水平,并作为PKA介导的底物磷酸化的调节剂发挥作用,导致钙可用性和肌丝钙敏感性发生变化。本综述的目的是阐明mAKAP作为一种支架蛋白在介导PKA信号传导和调节心肌细胞肥大中的关键区室化作用。基于我们的文献检索以及对AKAP支架蛋白与其结合伙伴之间结构-功能关系的研究,我们提出了mAKAP促进心脏肥大机制的可能解释。