Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2017-08-24 , DOI: 10.1016/j.bmc.2017.08.040 Miriam Fontanillo 1 , Maja Köhn 2
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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.
中文翻译：
微囊藻毒素：PP1 和 PP2A 的合成和构效关系研究
微囊藻毒素是引起植物、动物和人类中毒的剧毒蓝藻毒素。主要通过饮用水和受污染的食物接触微囊藻毒素是当前的世界健康问题。尽管非常具有挑战性，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性质并阐明它们与其主要靶蛋白磷酸酶-1 (PP1) 和 -2A (PP2A) 的结合机制。本综述侧重于制备微囊藻毒素和类似物的合成方法，并汇编了构效关系 (SAR) 研究，这些研究描述了微囊藻毒素的独特特性，这些特性使它们如此有效。
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