Solid-phase synthesis and biological evaluation of Joro spider toxin-4 from Nephila clavata

Publikation: Bidrag til tidsskriftTidsskriftartikelfagfællebedømt

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.
OriginalsprogEngelsk
TidsskriftJournal of Natural Products
Vol/bind74
Udgave nummer3
Sider (fra-til)483-486
ISSN0163-3864
DOI
StatusUdgivet - 2011

ID: 32318999