General synthesis of β-alanine-containing spider polyamine toxins and discovery of nephila polyamine toxins 1 and 8 as highly potent inhibitors of ion...
Basic Information
ID: ALA2176954
Journal: J Med Chem
Title: General synthesis of β-alanine-containing spider polyamine toxins and discovery of nephila polyamine toxins 1 and 8 as highly potent inhibitors of ionotropic glutamate receptors.
Authors: Lucas S, Poulsen MH, Nørager NG, Barslund AF, Bach TB, Kristensen AS, Strømgaard K.
Abstract: Certain spiders contain large pools of polyamine toxins, which are putative pharmacological tools awaiting further discovery. Here we present a general synthesis strategy for this class of toxins and prepare five structurally varied polyamine toxins. Electrophysiological testing at three ionotropic glutamate receptor subtypes reveals that two of these, Nephila polyamine toxins 1 (NPTX-1) and 8 (NPTX-8), comprise intriguing pharmacological activities by having subnanomolar IC(50) values at kainate receptors.
CiteXplore: 23092360
DOI: 10.1021/jm301255m
Patent ID: ┄