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AG 489 (or agatoxin 489) is a component of the
Both of these inhibit the TRPV1 channels from the extracellular membrane side. From the pore blocking mechanism, the pore mutations that change toxic affinity were identified. As a result, the four mutants decreased toxic affinity and several mutants increased it. Therefore, this was consistent with the scanned TM5-TM6 linker region being the outer vestibule of the channels and further confirming that AG489 is a pore blocker.
venom
Venom or zootoxin is a type of toxin produced by an animal that is actively delivered through a wound by means of a bite, sting, or similar action. The toxin is delivered through a specially evolved ''venom apparatus'', such as fangs or a sti ...
produced by ''Agelenopsis aperta
''Agelenopsis aperta'', also known as the desert grass spider or funnel-web spider, is a species of spider belonging to the family Agelenidae and the genus '' Agelenopsis''. It is found in dry and arid regions across the southern United States ...
'', a North American funnel web spider. It inhibits the ligand gated ion channel TRPV1 through a pore blocking mechanism.
Discovery
To identify new inhibitors, capsaicin receptor channels (TRPV1) were screened with a venom library for activity against these channels. In result, the robust inhibitory activity was found in the venom. Venom fractionation using reversed phaseHPLC
High-performance liquid chromatography (HPLC), formerly referred to as high-pressure liquid chromatography, is a technique in analytical chemistry used to separate, identify, and quantify specific components in mixtures. The mixtures can origina ...
allowed the purification of two acylpolyamine toxins, AG489 and AG505.
:
Both of these inhibit the TRPV1 channels from the extracellular membrane side. From the pore blocking mechanism, the pore mutations that change toxic affinity were identified. As a result, the four mutants decreased toxic affinity and several mutants increased it. Therefore, this was consistent with the scanned TM5-TM6 linker region being the outer vestibule of the channels and further confirming that AG489 is a pore blocker.
See also
*Agatoxin
Agatoxins are a class of chemically diverse polyamine and peptide toxins which are isolated from the venom of various spiders. Their mechanism of action includes blockade of glutamate -gated ion channels, voltage-gated sodium channels, or volta ...
References
External links
* {{MeshName, AG+489 Spider toxins Indoles Hydroxylamines Polyamines