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.
Originalsprog | Engelsk |
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Tidsskrift | Journal of Natural Products |
Vol/bind | 74 |
Udgave nummer | 3 |
Sider (fra-til) | 483-486 |
ISSN | 0163-3864 |
DOI | |
Status | Udgivet - 2011 |
- Det tidligere Farmaceutiske Fakultet
Forskningsområder
ID: 32318999