saxitoxin and maleimide

saxitoxin has been researched along with maleimide* in 1 studies

Other Studies

1 other study(ies) available for saxitoxin and maleimide

ArticleYear
Maleimide conjugates of saxitoxin as covalent inhibitors of voltage-gated sodium channels.
    Journal of the American Chemical Society, 2013, Jul-24, Volume: 135, Issue:29

    (+)-Saxitoxin, a naturally occurring guanidinium poison, functions as a potent, selective, and reversible inhibitor of voltage-gated sodium ion channels (NaVs). Modified forms of this toxin bearing cysteine-reactive maleimide groups are available through total synthesis and are found to irreversibly inhibit sodium ion conductance in recombinantly expressed wild-type sodium channels and in hippocampal nerve cells. Our findings support a mechanism for covalent protein modification in which toxin binding to the channel pore precedes maleimide alkylation of a nucleophilic amino acid. Second-generation maleimide-toxin conjugates, which include bioorthogonal reactive groups, are also found to block channel function irreversibly; such compounds have potential as reagents for selective labeling of NaVs for live cell imaging and/or proteomics experiments.

    Topics: Animals; CHO Cells; Cricetulus; Humans; Maleimides; Models, Molecular; Neurons; Rats; Saxitoxin; Sodium Channel Blockers; Sodium Channels

2013