Original Fluorescent Ligand-Based Assays Open New Perspectives in G-Protein Coupled Receptor Drug Screening
Original Fluorescent Ligand-Based Assays Open New Perspectives in G-Protein Coupled Receptor Drug Screening
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DOI：
10.3390/ph4010202
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发表时间：
2011-01-18
期刊：
影响因子：
4.6
通讯作者：
Durroux T
中科院分区：
文献类型：
--
作者：
Cottet M;Faklaris O;Zwier JM;Trinquet E;Pin JP;Durroux T
鉴别出副作用较小的新药是今后十年的一大挑战。筛选良好的候选配体需要许多步骤，其中之一就是评估它们的结合特性。基于荧光测量的新策略是传统放射性测定的极好替代品。这些方法危害更小，速度更快，成本更低，而且具有非常好的灵敏度，可用于各种生物模型，如异源表达系统或原生组织。
The identification of new drugs exhibiting reduced adverse side-effects constitutes a great challenge for the next decade. Various steps are needed to screen for good ligand candidates and one of them is the evaluation of their binding properties. New strategies based on fluorescence measurement constitute excellent alternatives to the traditional radioactive assays. Less hazardous, faster and cheaper, these methods also exhibit very good sensitivity and can be used on various biological models such as heterologous expression systems or native tissues.