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

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningfagfællebedømt

Anne Fuglsang Barslund, Mette Homann Poulsen, Tinna Brøbech Bach, Simon Lucas, Anders Skov Kristensen, Kristian Strømgaard

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