Genome Biology Unit, European Molecular Biology Laboratory (EMBL), Meyerhofstrasse 1, 69117 Heidelberg, Germany.
Genome Biology Unit, European Molecular Biology Laboratory (EMBL), Meyerhofstrasse 1, 69117 Heidelberg, Germany; Centre for Biological Signalling Studies (BIOSS), University of Freiburg, Schänzlestrasse 18, 79104 Freiburg, Germany; Faculty of Biology, University of Freiburg, Schänzlestrasse 1, 79104 Freiburg, Germany.
Bioorg Med Chem. 2018 Mar 15;26(6):1118-1126. doi: 10.1016/j.bmc.2017.08.040. Epub 2017 Aug 24.
Microcystins are highly toxic cyanotoxins responsible for plant, animal and human poisoning. Exposure to microcystins, mainly through drinkable water and contaminated food, is a current world health concern. Although it is quite challenging, the synthesis of these potent cyanotoxins, analogs and derivatives helps to evaluate their toxicological properties and to elucidate their binding mechanisms to their main targets Protein Phosphatase-1 (PP1) and -2A (PP2A). This review focuses on synthetic approaches to prepare microcystins and analogs and compiles structure-activity relationship (SAR) studies that describe the unique features of microcystins that make them so potent.
微囊藻毒素是一种高毒性的蓝藻毒素，可导致植物、动物和人类中毒。暴露于微囊藻毒素中，主要通过饮用水和受污染的食物，是当前全球关注的健康问题。尽管这极具挑战性，但这些强效蓝藻毒素、类似物和衍生物的合成有助于评估它们的毒理学特性，并阐明它们与主要靶标蛋白磷酸酶-1（PP1）和 -2A（PP2A）的结合机制。本综述重点介绍了制备微囊藻毒素和类似物的合成方法，并汇编了描述微囊藻毒素独特特征使其如此有效的结构-活性关系（SAR）研究。
