Division of Rheumatology, Department of Medicine, University of Padua, Via Giustiniani 2, 35128, Padua, Italy.
Clin Rev Allergy Immunol. 2013 Oct;45(2):267-80. doi: 10.1007/s12016-013-8353-3.
Serine protease inhibitors (serpins) are evolutionary old, structurally conserved molecules which encompass nearly all branches of life. More than 1,000 serpins were characterized to date which are subdivided into 16 subgroups (A-P) according to their common ancestry; among them, 37 are found in humans. Serpins were termed after their capability to inhibit serine proteases, but mounting evidence suggests that they may achieve a greater deal of functions, ranging from embryological growth to synaptic plasticity, development of both myeloid and lymphoid immune cells, and modulation of apoptosis. Serpins are mainly extracellular molecules, although some of them (namely, ov-serpins or clade B serpins) mostly act inside the cells, being either ubiquitously or tissue-specifically expressed. Among newly characterized serpin functions, regulation of cellular proliferation through apoptosis modulation and proteasome disturbance seems to play a major role. Accordingly, several serpins were found to be hyperexpressed in tumor cells. Indeed, apoptosis dysregulation is likely to be a cornerstone in both tumorigenesis and autoimmunity, since uncontrolled cellular viability results in tumor proliferation, while inefficient disposal of apoptotic debris may favor the rescue of autoreactive immune cells. Such a process was widely documented in systemic lupus erythematosus (SLE). Interestingly, alterations in the expression of some serpins, e.g., the ov-serpin SERPINB3, are being unraveled in patients affected with SLE and other autoimmune disorders, suggesting that a failure in serpin function might affect immune homeostasis and self-tolerance, thereby contributing to autoimmunity. Here, we provide an overview of serpin origin, function, and dysfunction, focusing on human serpins and ov-serpins, with a hub on SERPINB3.
丝氨酸蛋白酶抑制剂(serpins)是进化古老、结构保守的分子,几乎涵盖了所有生命的分支。迄今为止,已经有超过 1000 种 serpins 被鉴定出来,根据它们的共同祖先分为 16 个亚组(A-P);其中 37 种存在于人类中。serpins 之所以得名,是因为它们能够抑制丝氨酸蛋白酶,但越来越多的证据表明,它们可能具有更多的功能,从胚胎生长到突触可塑性、髓系和淋巴免疫细胞的发育,以及细胞凋亡的调节。serpins 主要是细胞外分子,尽管其中一些(即 ov-serpins 或 clade B serpins)主要在细胞内起作用,广泛或组织特异性表达。在新鉴定的 serpin 功能中,通过凋亡调节和蛋白酶体干扰调节细胞增殖似乎起着主要作用。因此,在肿瘤细胞中发现了几种 serpins 的过度表达。事实上,凋亡失调可能是肿瘤发生和自身免疫的基石,因为细胞活力不受控制会导致肿瘤增殖,而凋亡碎片处理效率低下可能有利于自身反应性免疫细胞的挽救。这种过程在系统性红斑狼疮(SLE)中得到了广泛的证明。有趣的是,一些 serpins 的表达改变,例如 ov-serpin SERPINB3,在患有 SLE 和其他自身免疫性疾病的患者中被揭示出来,这表明 serpin 功能的失败可能会影响免疫稳态和自身耐受性,从而导致自身免疫。在这里,我们提供了 serpin 起源、功能和功能障碍的概述,重点是人类 serpins 和 ov-serpins,并以 SERPINB3 为中心。