Vorozhtsov Institute of Organic Chemistry, Siberian Division, Russian Academy of Sciences, pr. akademika Lavrent'eva 9 Novosibirsk, 630090, Russian Federation.
Curr Med Chem. 2011;18(26):4076-105. doi: 10.2174/092986711796957248.
This review is the first attempt at systematization and analysis of the literature data (covering the last decade) on the chemical structures and specific activities of cholesterol-regulating agents. Six of thirty currently known biological targets for treating hyperlipidemia were selected and considered. All of the chemical structures under study are divided into two classes with different mechanisms of their activity: cholesterol biosynthesis blockers (HMG-CoA reductase and squalene 2,3-oxide-lanosterol cyclase inhibitors) and regulators of cholesterol transformations in the organism (PPARα and PPARα/γ agonists, inhibitors of intestinal absorption of cholesterol, cholesteryl ester transfer protein (CETP) inhibitors, and regulators of low-density-lipoprotein receptor (LDLR) expression).
这是首次对过去十年间有关调节胆固醇的试剂的化学结构和特定活性的文献资料进行系统化和分析。本文选取了六种目前已知的治疗高血脂的生物靶点进行研究。所有研究的化学结构被分为两类，其活性机制不同：胆固醇生物合成抑制剂（HMG-CoA 还原酶和鲨烯 2,3-氧化物-羊毛甾醇环化酶抑制剂）和调节体内胆固醇转化的试剂（PPARα 和 PPARα/γ激动剂、胆固醇吸收抑制剂、胆固醇酯转移蛋白（CETP）抑制剂和调节低密度脂蛋白受体（LDLR）表达的试剂）。
