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in which the activation sequence normally recognized by plasmin (Pro-Arg-Phe-Lys upward arrowIle-Ile-Gly-Gly) has been replaced by a sequence expected to be recognized and hydrolysed by many MMPs (Arg-Pro-Leu-Gly upward arrowIle-Ile-Gly-Gly).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

我们描述了一种评估所有类别蛋白水解酶活性的新原理,并展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。这一新原理的核心是存在一种原酶,该原酶可以通过一次蛋白水解事件被激活为活性酶。使用蛋白质工程技术将原酶中的常规激活序列替换为待确定的蛋白酶识别的人工序列。后者可以作为新改造的原酶的激活剂。在本文中,基于此原理描述了一种用于确定MMPs的简单比色测定法。借助蛋白质工程,已经制备了一种改良的尿激酶原,其中通常由纤溶酶识别的激活序列 (pro-Arg-Phe-Lys向上arrowIle-Ile-Gly) 已被预期被许多MMPs识别和水解的序列所取代 (Arg-Pro-Leu-Gly向上arrowIle-ile-Gly)。通过MMP激活修饰的尿激酶原而产生的活性尿激酶可以直接,使用尿激酶的特定显色肽底物进行测量,也可以通过尿激酶催化的纤溶酶原活化间接测量。测定对相等摩尔量的活性mmp的响应以MMP-2>MMP-9>MMP-1>MMP-3>MMP-7的顺序降低。MMP-9的检测限低于15μm,对应于3。每项测定75x10(-15) 摩尔。使用该测定法,类风湿关节炎患者的滑膜组织提取物与骨关节炎患者的滑膜组织提取物相比,以及与正常胃组织提取物相比,胃肿瘤提取物中的MMP活性增加。

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