We describe a new principle for assessment of the activity of proteolytic enzymes of all classes and show the application of this principle for the quantitative assay of bacterial collagenase and human matrix metalloproteinases (MMPs). Central to this new principle is the presence of a proenzyme that can be activated into an active enzyme by a single proteolytic event. The regular activation sequence in the proenzyme is replaced using protein engineering by an artificial sequence recognized by the proteinase to be determined. The latter can act as an activator for the newly engineered proenzyme. In the present paper a simple colorimetric assay for the determination for MMPs is described based on this principle. With the aid of protein engineering, a modified pro-urokinase has been prepared in which the activation sequence normally recognized by plasmin (Pro-Arg-Phe-Lys upward arrowIle-Ile-Gly-Gly) has been replaced by a sequence expected to be recognized and hydrolysed by many MMPs (Arg-Pro-Leu-Gly upward arrowIle-Ile-Gly-Gly). The active urokinase resulting from activation of the modified pro-urokinase by a MMP could be measured either directly, using a specific chromogenic peptide substrate for urokinase, or indirectly via urokinase-catalysed plasminogen activation. The response of the assay to equal molar quantities of active MMPs decreases in the order MMP-2>MMP-9>MMP-1>MMP-3>MMP-7. The detection limit for MMP-9 was below 15 pM, corresponding to 3. 75x10(-15) mol per assay. Using the assay, increased MMP activity was detected in synovial tissue extracts from rheumatoid arthritis patients compared with those from osteoarthritis patients, and in stomach tumour extracts as compared with normal stomach tissue extracts.

译文

我们描述了评估所有类别蛋白水解酶活性的新原理,并显示了该原理在细菌胶原酶和人类基质金属蛋白酶(MMPs)定量测定中的应用。这个新原理的核心是存在一种可以通过单个蛋白水解事件激活为活性酶的酶。使用蛋白质工程技术,用待确定的蛋白酶识别的人工序列代替原酶中的常规激活序列。后者可以充当新设计的酶的激活剂。在本文中,基于此原理描述了一种简单的比色测定法,用于测定MMP。借助于蛋白质工程,已经制备了修饰的尿激酶原,其中通常被纤溶酶识别的激活序列(Pro-Arg-Phe-Lys向上箭头Ile-Ile-Gly-Gly)被替换为预期的序列。被许多MMP(Arg-Pro-Leu-Gly向上箭头Ile-Ile-Gly-Gly)识别和水解。可以通过使用尿激酶的特定生色肽底物直接测量由MMP激活修饰的尿激酶原而激活的活性尿激酶,或通过尿激酶催化的纤溶酶原激活间接测量。测定法对等摩尔量的活性MMP的响应以MMP-2> MMP-9> MMP-1> MMP-3> MMP-7的顺序降低。 MMP-9的检出限低于15 pM,对应于每次测定3. 75 x10(-15)mol。使用该测定法,与类骨关节炎患者相比,类风湿性关节炎患者的滑膜组织提取物和正常胃组织提取物中的MMP活性均升高。

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