利用特异性来策略性地靶向蛋白酶。
Using specificity to strategically target proteases.
作者信息
Lim Mark D, Craik Charles S
机构信息
Department of Pharmaceutical Chemistry, University of California, School of Pharmacy, 513 Parnassus Avenue Room S-926, San Francisco, CA 94158, USA.
出版信息
Bioorg Med Chem. 2009 Feb 1;17(3):1094-100. doi: 10.1016/j.bmc.2008.03.068. Epub 2008 Mar 30.
Abstract
Proteases are a family of naturally occurring enzymes in the body whose dysregulation has been implicated in numerous diseases and cancers. Their ability to selectively and catalytically turnover substrate adds both signal amplification and functionality as parameters for the detection of disease. This review will focus on the development of activity-based methodologies to characterize proteases, and in particular, the use of positional scanning, synthetic combinatorial libraries (PS-SCL's), and substrate activity screening (SAS) assays. The use of these approaches to better understand a protease's natural substrate will be discussed as well as the technologies that emerged.
摘要
蛋白酶是人体中天然存在的一类酶，其失调与多种疾病和癌症有关。它们选择性地催化底物周转的能力增加了信号放大和功能，作为疾病检测的参数。本综述将重点关注基于活性的蛋白酶表征方法的发展，特别是位置扫描、合成组合文库（PS-SCL）和底物活性筛选（SAS）测定法的应用。还将讨论如何使用这些方法更好地了解蛋白酶的天然底物以及由此产生的技术。
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