Novosibirsk Institute of Chemical Biology and Fundamental Medicine, Siberian Branch of the Russian Academy of Sciences, Prospect Lavrentieva 8, Novosibirsk, 630090, Russia.
Med Chem. 2012 Sep;8(5):883-93. doi: 10.2174/157340612802084225.
The influence of a number of usnic acid derivatives on auto(polyADP-ribosyl)ation catalyzed by PARP1 and DNA synthesis catalyzed by DNA polymerase β was studied. The derivatives of usnic acid containing aromatic substituents were shown to be moderate inhibitors of PARP1. The presence of both usnic acid tricyclic structure and aromatic substituent at any position of the molecule is a key factor for the inhibitory action. In the case of DNA polymerase β, no relationship between the structure and inhibitory properties has been found with the only exception. Derivatives with modified ring A showed mild activation of DNA synthesis catalyzed by DNA polymerase β.
研究了几种地衣酸衍生物对 PARP1 催化的自动（多 ADP-核糖基）化和 DNA 聚合酶 β 催化的 DNA 合成的影响。含有芳香取代基的地衣酸衍生物被证明是 PARP1 的中等抑制剂。分子中任何位置的地衣酸三环结构和芳香取代基的存在是抑制作用的关键因素。对于 DNA 聚合酶 β，除了一个例外，没有发现结构和抑制特性之间的关系。具有修饰的环 A 的衍生物对 DNA 聚合酶 β 催化的 DNA 合成表现出温和的激活作用。
