Department of Chemistry, Chemistry Research Laboratory, University of Oxford, Mansfield Road, Oxford, OX1 3TA, UK.
J Am Chem Soc. 2010 Mar 17;132(10):3238-9. doi: 10.1021/ja909165u.
The identification, synthesis, and evaluation of a series of naphthoquinone derivatives as selective inhibitors of human arylamine N-acetyltransferase 1 and mouse arylamine N-acetyltransferase 2 are described. The compounds undergo a distinctive color change (red --> blue) upon binding to these human and mouse NAT isoenzymes driven by a proton transfer event. No color change is observed in the presence of functionally distinct but highly similar isoenzymes which are >70% identical. These molecules may be used as sensors to detect the presence of human NAT1 in cell lysates.
本文描述了一系列萘醌衍生物作为人芳香胺 N-乙酰转移酶 1 和鼠芳香胺 N-乙酰转移酶 2 的选择性抑制剂的鉴定、合成和评估。这些化合物与这些人和鼠 NAT 同工酶结合后，会发生独特的颜色变化（红-蓝），这是由质子转移事件驱动的。在存在功能不同但高度相似的同工酶（相似度>70%）的情况下，不会观察到颜色变化。这些分子可用作传感器来检测细胞裂解物中是否存在人 NAT1。
