Vertebrate and invertebrate ligand-gated ion channels (LGICs) exhibit significant structural homology and often share ligands. As a result, ligands with activity against one class can be brought to bear against another, including for development as insecticides. Receptor selectivity, metabolism and distribution must then be optimized using chemical synthesis. Here we review natural products (NPs) that ligate and inhibit the Cys-loop family of LGICs, which benefit from the unique physicochemical properties of natural product space but often present a high synthetic burden. Recent advances in chemical synthesis, however, have opened practical entries into these complex structures, several of which are highlighted. © 2020 Society of Chemical Industry

中文翻译：

---

改变通道：来自大自然的 CysLoop 受体拮抗剂

脊椎动物和无脊椎动物配体门控离子通道 (LGIC) 具有显着的结构同源性，并且经常共享配体。结果，具有针对一类活性的配体可以用于对抗另一类，包括开发为杀虫剂。然后必须使用化学合成优化受体选择性、代谢和分布。在这里，我们回顾了连接和抑制 LGIC 的 Cys-loop 家族的天然产物 (NPs)，它们受益于天然产物空间的独特物理化学特性，但通常会带来很高的合成负担。然而，化学合成的最新进展已经为这些复杂结构打开了实用的入口，其中一些被突出显示。© 2020 化工学会