The Second Department of General Surgery, Zhuhai People's Hospital, No. 79 of Kangning Road, Xiangzhou District, Zhuhai City, Guangdong Province, China.
The Second Department of General Surgery, Zhuhai People's Hospital, No. 79 of Kangning Road, Xiangzhou District, Zhuhai City, Guangdong Province, China.
Arch Med Res. 2018 Oct;49(7):423-429. doi: 10.1016/j.arcmed.2019.02.004. Epub 2019 Mar 6.
As we all know, heparanase plays an important role in human diseases. As a kind of endo-β-glucuronidase, heparanase is the known only enzyme in mammals which could degrade heparan sulfate(HS) specifically. HS is a vital component of extracellular matrix(ECM). Heparanase takes effect by cleaving theβ(1,4)-glycosidic between glucosamine residue and glucuronic acid of HS. This cleavage will cause ECM remodelling and HS-linked biological molecules release, including cytokines, growth factors and a lot of biological molecules regulating various pathological activities. Experiments already proved that heparanase gene over-expresses in cancers of gastrointestinal tract, esophagus, breast and so on. Various studies have demonstrated the heparanase's pro-metastatic function and the reduced survival rate of patients could be indicated by high heparanase levels. Besides, pathological processes including procoagulant activities, preeclamptic placentas and inflammation are all verified to be associated with heparanase activity. In recent years, many functions other than pro-tumor effect was found in heparanase and worldwide researchers conducted varieties of experiments to identify the new function of this significant enzyme. Also, these newly-found functions are closely connected to certain cellular activities, for example epithelial to mesenchymal transition (EMT). It has already been demonstrated that EMT is related to some clinical disorders, like renal diseases. Given that heparanase is the only enzyme capable of this function, it could be concluded that heparanase would be a potential and valuable therapy target. This mini-review aims to retrospect literatures about heparanase published in 2017 and 2018 and provide a direction for therapy methods targeting heparanase.
众所周知,肝素酶在人类疾病中起着重要作用。作为一种内-β-葡糖醛酸酶,肝素酶是哺乳动物中已知的唯一能够特异性降解硫酸乙酰肝素 (HS) 的酶。HS 是细胞外基质 (ECM) 的重要组成部分。肝素酶通过裂解 HS 中葡萄糖胺残基和葡萄糖醛酸之间的β(1,4)-糖苷键发挥作用。这种裂解会导致 ECM 重塑和 HS 连接的生物分子释放,包括细胞因子、生长因子和许多调节各种病理活动的生物分子。实验已经证明,肝素酶基因在胃肠道、食管、乳腺等癌症中过度表达。各种研究表明肝素酶具有促转移功能,高肝素酶水平可提示患者生存率降低。此外,包括促凝活性、子痫前期胎盘和炎症在内的病理过程都被证实与肝素酶活性有关。近年来,肝素酶除了具有促肿瘤作用外,还发现了其他多种功能,全世界的研究人员都进行了各种实验来确定这种重要酶的新功能。此外,这些新发现的功能与某些细胞活动密切相关,例如上皮细胞向间充质转化 (EMT)。已经证明 EMT 与某些临床疾病有关,如肾脏疾病。鉴于肝素酶是唯一具有这种功能的酶,因此可以得出结论,肝素酶将是一个有潜力和有价值的治疗靶点。本综述旨在回顾 2017 年和 2018 年发表的关于肝素酶的文献,并为靶向肝素酶的治疗方法提供一个方向。