XB-ART-43353
J Nat Prod
2011 Mar 25;743:483-6. doi: 10.1021/np100746w.
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Solid-phase synthesis and biological evaluation of Joro spider toxin-4 from Nephila clavata.
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Polyamine toxins from orb weaver spiders are attractive pharmacological tools particularly for studies of ionotropic glutamate (iGlu) receptors in the brain. These polyamine toxins are biosynthesized in a combinatorial manner, providing a plethora of related, but structurally complex toxins to be exploited in biological studies. Here, we have used solid-phase synthetic methodology for the efficient synthesis of Joro spider toxin-4 (JSTX-4) (1) from Nephila clavata, providing sufficient amounts of the toxin for biological evaluation at iGlu receptor subtypes using electrophysiology. Biological evaluation revealed that JSTX-4 inhibits iGlu receptors only in high μM concentrations, thereby being substantially less potent than structurally related polyamine toxins.
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