A fluopol-ABPP HTS assay to identify PAD inhibitors.

A fluopol-ABPP HTS assay to identify PAD inhibitors.
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DOI:
10.1039/c0cc02634d
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发表时间:
2010-10-14
期刊:
Chemical communications (Cambridge, England)
影响因子:
--
通讯作者:
Thompson PR
Thompson PR
中科院分区:
其他
文献类型:
--
作者:
Knuckley B;Jones JE;Bachovchin DA;Slack J;Causey CP;Brown SJ;Rosen H;Cravatt BF;Thompson PR

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蛋白质精氨酸脱亚胺酶(PAD)活性在许多疾病中失调,例如,类风湿关节炎在此,我们描述了一种基于荧光偏振活性的蛋白质谱(fluopol-ABPP)的高通量筛选试验,可用于识别PAD选择性抑制剂的发展。使用该测定,链黑菌素被鉴定为有效的、选择性的和不可逆的PAD 4灭活剂。
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