Department of Pharmacognosy-Pharmacology, School of Pharmacy, Aristotle University of Thessaloniki, 541 24, Thessaloniki, Greece.
Department of Pharmacy, School of Health Sciences, University of Patras, 265 04, Rion-Patras, Greece.
Cell Mol Life Sci. 2021 Nov;78(21-22):6735-6744. doi: 10.1007/s00018-021-03922-7. Epub 2021 Aug 30.
Kallikrein-related peptidases (KLKs) or kallikreins have been linked to diverse (patho) physiological processes, such as the epidermal desquamation and inflammation, seminal clot liquefaction, neurodegeneration, and cancer. Recent mounting evidence suggests that KLKs also represent important regulators of viral infections. It is well-established that certain enveloped viruses, including influenza and coronaviruses, require proteolytic processing of their hemagglutinin or spike proteins, respectively, to infect host cells. Similarly, the capsid protein of the non-enveloped papillomavirus L1 should be proteolytically cleaved for viral uncoating. Consequently, extracellular or membrane-bound proteases of the host cells are instrumental for viral infections and represent potential targets for drug development. Here, we summarize how extracellular proteolysis mediated by the kallikreins is implicated in the process of influenza (and potentially coronavirus and papillomavirus) entry into host cells. Besides direct proteolytic activation of viruses, KLK5 and 12 promote viral entry indirectly through proteolytic cascade events, like the activation of thrombolytic enzymes that also can process hemagglutinin, while additional functions of KLKs in infection cannot be excluded. In the light of recent evidence, KLKs represent potential host targets for the development of new antivirals. Humanized animal models to validate their key functions in viral infections will be valuable.
激肽释放酶相关肽酶(KLKs)或激肽释放酶与多种(病理)生理过程有关,如表皮脱屑和炎症、精液凝块液化、神经退行性变和癌症。最近越来越多的证据表明,KLKs 也是病毒感染的重要调节剂。众所周知,某些包膜病毒,包括流感病毒和冠状病毒,分别需要对其血凝素或刺突蛋白进行蛋白水解处理,才能感染宿主细胞。同样,无包膜的乳头瘤病毒 L1 的衣壳蛋白也应该通过蛋白水解切割进行病毒脱壳。因此,宿主细胞的细胞外或膜结合蛋白酶对于病毒感染至关重要,并且是药物开发的潜在靶点。在这里,我们总结了细胞外蛋白水解介导的激肽释放酶如何参与流感(以及潜在的冠状病毒和乳头瘤病毒)进入宿主细胞的过程。除了直接的病毒蛋白水解激活作用外,KLK5 和 12 通过蛋白水解级联事件间接促进病毒进入,例如激活纤溶酶,纤溶酶也可以处理血凝素,而 KLKs 在感染中的其他功能不能排除。鉴于最近的证据,KLKs 代表了开发新型抗病毒药物的潜在宿主靶点。验证它们在病毒感染中的关键功能的人源化动物模型将是有价值的。