Stracina T, Novakova M
Department of Physiology, Faculty of Medicine, Masaryk University, Brno, Czech Republic.
Physiol Res. 2018 Dec 31;67(Suppl 4):S561-S576. doi: 10.33549/physiolres.934052.
More than four decades passed since sigma receptors were first mentioned. Since then, existence of at least two receptor subtypes and their tissue distributions have been proposed. Nowadays, it is clear, that sigma receptors are unique ubiquitous proteins with pluripotent function, which can interact with so many different classes of proteins. As the endoplasmic resident proteins, they work as molecular chaperones - accompany various proteins during their folding, ensure trafficking of the maturated proteins between cellular organelles and regulate their functions. In the heart, sigma receptor type 1 is more dominant. Cardiac sigma 1 receptors regulate response to endoplasmic reticulum stress, modulates calcium signaling in cardiomyocyte and can affect function of voltage-gated ion channels. They contributed in pathophysiology of cardiac hypertrophy, heart failure and many other cardiovascular disorders. Therefore, sigma receptors are potential novel targets for specific treatment of cardiovascular diseases.
自首次提及西格玛受体以来,四十多年过去了。从那时起,人们提出了至少两种受体亚型的存在及其组织分布。如今,很明显,西格玛受体是具有多能功能的独特的普遍存在的蛋白质,它可以与许多不同类别的蛋白质相互作用。作为内质网驻留蛋白,它们充当分子伴侣——在各种蛋白质折叠过程中陪伴它们,确保成熟蛋白质在细胞器之间的运输并调节其功能。在心脏中,1型西格玛受体更为占主导地位。心脏西格玛1受体调节对内质网应激的反应,调节心肌细胞中的钙信号传导,并可影响电压门控离子通道的功能。它们在心脏肥大、心力衰竭和许多其他心血管疾病的病理生理学中起作用。因此,西格玛受体是心血管疾病特异性治疗的潜在新靶点。