Department of Neuroscience, Rosalind Franklin University/The Chicago Medical School, 3333 Green Bay Road, North Chicago, IL 60064, USA.
Pharmacol Rev. 2011 Sep;63(3):700-27. doi: 10.1124/pr.110.003814. Epub 2011 Jul 7.
The endoplasmic reticulum (ER) is a morphologically and functionally diverse organelle capable of integrating multiple extracellular and internal signals and generating adaptive cellular responses. It plays fundamental roles in protein synthesis and folding and in cellular responses to metabolic and proteotoxic stress. In addition, the ER stores and releases Ca(2+) in sophisticated scenarios that regulate a range of processes in excitable cells throughout the body, including muscle contraction and relaxation, endocrine regulation of metabolism, learning and memory, and cell death. One or more Ca(2+) ATPases and two types of ER membrane Ca(2+) channels (inositol trisphosphate and ryanodine receptors) are the major proteins involved in ER Ca(2+) uptake and release, respectively. There are also direct and indirect interactions of ER Ca(2+) stores with plasma membrane and mitochondrial Ca(2+)-regulating systems. Pharmacological agents that selectively modify ER Ca(2+) release or uptake have enabled studies that revealed many different physiological roles for ER Ca(2+) signaling. Several inherited diseases are caused by mutations in ER Ca(2+)-regulating proteins, and perturbed ER Ca(2+) homeostasis is implicated in a range of acquired disorders. Preclinical investigations suggest a therapeutic potential for use of agents that target ER Ca(2+) handling systems of excitable cells in disorders ranging from cardiac arrhythmias and skeletal muscle myopathies to Alzheimer disease.
内质网(ER)是一种形态和功能多样化的细胞器,能够整合多种细胞外和细胞内信号,并产生适应性的细胞反应。它在蛋白质合成和折叠以及细胞对代谢和蛋白毒性应激的反应中起着重要作用。此外,内质网在复杂的情况下储存和释放 Ca(2+),调节身体中各种兴奋细胞的一系列过程,包括肌肉收缩和松弛、代谢的内分泌调节、学习和记忆以及细胞死亡。一个或多个 Ca(2+)ATP 酶和两种类型的内质网膜 Ca(2+)通道(三磷酸肌醇和兰尼碱受体)分别是参与内质网 Ca(2+)摄取和释放的主要蛋白。内质网 Ca(2+)储存还与质膜和线粒体 Ca(2+)调节系统有直接和间接的相互作用。选择性修饰内质网 Ca(2+)释放或摄取的药理学试剂使能够进行研究,揭示内质网 Ca(2+)信号的许多不同的生理作用。几种遗传性疾病是由内质网 Ca(2+)调节蛋白的突变引起的,内质网 Ca(2+)稳态的紊乱与一系列获得性疾病有关。临床前研究表明,靶向兴奋细胞内质网 Ca(2+)处理系统的药物在心律失常和骨骼肌肌病到阿尔茨海默病等疾病中具有治疗潜力。