基质金属蛋白酶

基质金属蛋白酶是一类分解细胞外基质组分的锌蛋白酶⒚它们在有机体生长发育中的细胞外基质逆转与重塑以及疾病中的病理损害起着极为重要的作用⒚基质金属蛋白酶的表达和活性在不同细胞水平受到严密调控，如细胞因子、生长因子以及激素的调节⒚基质金属蛋白酶以酶原形式分泌，随后被其它蛋白酶如胞浆素或非蛋白酶类化学物质如有机汞所激活⒚所有基质金属蛋白酶都受到天然抑制剂 金属蛋白酶组织抑制剂所抑制⒚两者的不平衡导致许多疾病的发生，如肿瘤侵入及转移⒚合成基质金属蛋白酶组织抑制剂所抑制，如 Ｍ ａｒｉｍ ａｓｔａｔ 能控制肿瘤转移的发生及进一步扩散⒚本文将对基质金属蛋白酶的特征、分子区域结构、底物特性、激活机制、调控方式等方面进行最新概述⒚

Matrix Metalloproteinases

Matrix metalloproteinases (MMPs) are zinc proteinases that degrade compounds of the extracellular matrix (ECM). These enzymes play a pivotal role in turnover and re modelling of the ECM during organism growth and development and the pathological destruction of tissues in diseases. The activities of metalloproteinases are tightly con trolled at several different cellular levels such as modulation by cytokines, growth factors and hormones. MMPs are secreted as zymogens which can be activated by other proteinas es such as plasmin or non proteolytic agents such as organomercurials. All MMPs are in hibited by their natural inhibitors, tissue inhibitors of matrix metalloproteinases (TIMPs). Imbalance between MMPs and TIMPs has been implicated in many diseases such as tumour invasion and metastasis. The synthetic MMP inhibitors such as Marimastat can prevent the growth and further spread of established metastases.