AG 489
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AG 489 (or agatoxin 489) is a component of the
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 ''Agelenopsis'', commonly known as the American grass spiders, is a genus of funnel weavers first described by C.G. Giebel in 1869. They weave sheet webs that have a funnel shelter on one edge. The web is not sticky, but these spiders make up fo ...
aperta, a North American funnel web spider. It inhibits the
ligand gated ion channel Ligand-gated ion channels (LICs, LGIC), also commonly referred to as ionotropic receptors, are a group of transmembrane ion-channel proteins which open to allow ions such as Na+, K+, Ca2+, and/or Cl− to pass through the membrane in res ...
TRPV1 The transient receptor potential cation channel subfamily V member 1 (TrpV1), also known as the capsaicin receptor and the vanilloid receptor 1, is a protein that, in humans, is encoded by the ''TRPV1'' gene. It was the first isolated member of th ...
through a pore blocking mechanism. To identify new inhibitors, capsaicin receptor channels (TRPV1) were screened from a venom library for activity against these channels. In result, the robust inhibitory activity was found in the venom. Venom fractionation utilizing a reversed phase HPLC which led to the purification of the 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 voltage- ...


References


External links

* Spider toxins {{biochem-stub