Effect of detergent on "promiscuous" inhibitors

Effect of detergent on "promiscuous" inhibitors
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DOI:
10.1021/jm0340896
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发表时间:
2003-07-31
影响因子:
7.3
通讯作者:
Chung, CW
Chung, CW
中科院分区:
医学1区
文献类型:
--
作者:
Ryan, AJ;Gray, NM;Chung, CW

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术语“混杂的”抑制剂是指其抑制机制涉及许多化合物分子的聚集体与靶蛋白的相互作用,而不是单个分子的结合的化合物。本文表明,混杂抑制剂可以区分从经典的1:1抑制剂的明智使用的洗涤剂,使之有可能配置检测,显着减少这种不良的抑制机制,而不损害检测性能。
The term "promiscuous" inhibitors has been coined for compounds whose inhibition mechanism involves the interaction of aggregates of many compound molecules with the target protein, rather than the binding of individual molecules. This paper demonstrates that promiscuous inhibitors can be differentiated from classical 1:1 inhibitors by the judicious use of detergents, making it possible to configure assays that significantly reduce this undesirable mechanism of inhibition without compromising assay performance.