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Change the channel: CysLoop receptor antagonists from nature
Author(s) -
Tong Guanghu,
Baker Meghan A,
Shenvi Ryan A
Publication year - 2021
Publication title -
pest management science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.296
H-Index - 125
eISSN - 1526-4998
pISSN - 1526-498X
DOI - 10.1002/ps.6166
Subject(s) - chemical space , natural product , computational biology , receptor , ligand (biochemistry) , biology , chemistry , chemical biology , chemical synthesis , biochemistry , drug discovery , in vitro
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