首页> 外文期刊>Journal of chromatography, B. Analytical technologies in the biomedical and life sciences >Immobilization of matrix metalloproteinase 8 (MMP-8) for online drug screening
【24h】

Immobilization of matrix metalloproteinase 8 (MMP-8) for online drug screening

机译:固定基质金属蛋白酶8(MMP-8)用于在线药物筛选

获取原文
获取原文并翻译 | 示例
       

摘要

Matrix metalloproteinase 8 (MMP-8) has been reported to have a key role in several pathologic conditions, like heart diseases, osteoarthritis, multiple sclerosis, and various other inflammatory conditions. Therefore, there is a great interest regarding the development of MMP-8 selective inhibitors. In the recent years, immobilized enzyme reactors (IMERs) proved to be an efficient alternative to solution-based assays. Besides the recycling of the enzyme, IMER approach allows a simple way to determine affinity data and thus the ranking of inhibiting potency of the compounds under study, especially when coupled to MS. In this study, the immobilization of MMP-8 was investigated in terms of type of support, kinetic parameters, storage and pH stability. Epoxy activated silica resulted the best matrix for the preparation of an immobilized enzyme reactor (IMER) containing human MMP-8. The IMER was successfully used for the online screening of known MMP-8 inhibitors in zonal chromatography and inhibition experiments.
机译:据报道,基质金属蛋白酶8(MMP-8)在几种病理状况中具有关键作用,例如心脏病,骨关节炎,多发性硬化症和各种其他炎症状况。因此,对MMP-8选择性抑制剂的开发非常感兴趣。近年来,固定化酶反应器(IMER)被证明是基于溶液的测定的有效替代方法。除了酶的循环利用外,IMER方法还提供了一种简单的方法来确定亲和力数据,从而确定所研究化合物的抑制效力(尤其是与MS偶联时)的排名。在这项研究中,从支持物的类型,动力学参数,储存和pH稳定性方面研究了MMP-8的固定化。环氧活化二氧化硅是制备含人MMP-8的固定化酶反应器(IMER)的最佳基质。 IMER已成功用于区域色谱和抑制实验中已知MMP-8抑制剂的在线筛选。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号