Mechanistic differences between in vitro assays for hydrazone-based small molecule inhibitors of anthrax lethal factor

Mechanistic differences between in vitro assays for hydrazone-based small molecule inhibitors of anthrax lethal factor
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DOI:
10.1016/j.bioorg.2006.07.004
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发表时间:
2007-02-01
影响因子:
5.1
通讯作者:
Perkins, Julie
Perkins, Julie
中科院分区:
化学1区
文献类型:
--
作者:
Hanna, M. Leslie;Tarasow, Theodore M.;Perkins, Julie

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系统生成的一系列腙被分析为炭疽致死因子的潜在抑制剂。使用一种基于紫外的体外测定和两种基于荧光的体外测定来筛选腙。该研究鉴定了几种 IC50 值在微摩尔范围内的抑制剂,重要的是,通过不同的测定观察到抑制类型的显着差异。 (c) 2006 Elsevier Inc. 保留所有权利。
A systematically generated series of hydrazones were analyzed as potential inhibitors of anthrax lethal factor. The hydrazones were screened using one UV-based and two fluorescence-based in vitro assays. The study identified several inhibitors with IC50 values in the micromolar range, and importantly, significant differences in the types of inhibition were observed with the different assays. (c) 2006 Elsevier Inc. All rights reserved.