Department of Chemistry, The Scripps Research Institute, Scripps Florida, 120 Scripps Way, Jupiter, Florida, USA33458.
Chem Commun (Camb). 2010 Oct 14;46(38):7175-7. doi: 10.1039/c0cc02634d. Epub 2010 Aug 25.
Protein Arginine Deiminase (PAD) activity is dysregulated in numerous diseases, e.g., Rheumatoid Arthritis. Herein we describe the development of a fluorescence polarization-Activity Based Protein Profiling (fluopol-ABPP) based high throughput screening assay that can be used to identify PAD-selective inhibitors. Using this assay, streptonigrin was identified as a potent, selective, and irreversible PAD4 inactivator.
蛋白质精氨酸脱亚氨酶（PAD）活性在许多疾病中失调，例如类风湿性关节炎。在此，我们描述了一种荧光偏振-基于活性的蛋白质谱分析（fluopol-ABPP）高通量筛选测定法的开发，该测定法可用于鉴定 PAD 选择性抑制剂。使用该测定法，链黑菌素被鉴定为一种有效的、选择性的、不可逆的 PAD4 失活剂。
