质谱技术在酶抑制剂筛选中的研究进展

Recent advances in enzyme inhibitor screening based on mass spectrometry

酶是调控人体机能使机体进行正常生命活动的物质,酶抑制剂能特异性调节酶的活性并可能成为药物发现的起点。目前,质谱具有对酶反应进行快速定量分析的优势,使其在酶抑制剂筛选发现新药领域发展迅猛。本文综述了近几年国内外应用质谱以及质谱联用技术(前沿亲和色谱、固定化酶磁珠、超滤、表面等离子体共振、毛细管电泳和微流控芯片)筛选酶抑制剂的方法。按照两种不同筛选原理进行阐述:活性筛选和亲和筛选。

Enzymes play crucial functional roles in all biological processes.Enzymatic inhibitors can regulate enzyme activity and may become the starting point for drug discovery.Mass spectrometry(MS)has the advantage for rapid qualitative and quantitative analyses of compounds and enzyme reactions,emerging as an important analytical tool in enzyme inhibitor screening assay for drug discovery.This review will highlight recent advances in the inhibitor screening assay using MS and related techniques,including frontier affinity chromatography,immobilized enzyme beads,ultrafiltration,surface plasmon resonance,capillary electrophoresis and microfluidic chips.The existing MS methods for screening enzyme inhibitor were divided into two types:affinity screening and activity screening.