2kgu

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Spatial structure of purotoxin-1 in waterSpatial structure of purotoxin-1 in water

Structural highlights

2kgu is a 1 chain structure with sequence from Alopecosa marikovskyi. Full experimental information is available from OCA. For a guided tour on the structure components use FirstGlance.
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

TXPR1_ALOMR Inhibits P2RX3 receptors. Has an analgesic effect in rat. Enhances the high-affinity desensitization of P2RX3 receptors. At 50 nM, decreases the IC(50) for ambient ATP from 46.5 nM to 12.7 nM in mouse P2RX3.[1] [2]

Publication Abstract from PubMed

P2X3 purinoreceptors expressed in mammalian sensory neurons play a key role in several processes, including pain perception. From the venom of the Central Asian spider Geolycosa sp., we have isolated a novel peptide, named purotoxin-1 (PT1), which is to our knowledge the first natural molecule exerting powerful and selective inhibitory action on P2X3 receptors. PT1 dramatically slows down the removal of desensitization of these receptors. The peptide demonstrates potent antinociceptive properties in animal models of inflammatory pain.

Novel peptide from spider venom inhibits P2X3 receptors and inflammatory pain.,Grishin EV, Savchenko GA, Vassilevski AA, Korolkova YV, Boychuk YA, Viatchenko-Karpinski VY, Nadezhdin KD, Arseniev AS, Pluzhnikov KA, Kulyk VB, Voitenko NV, Krishtal OO Ann Neurol. 2010 May;67(5):680-3. PMID:20437566[3]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

References

  1. Grishin EV, Savchenko GA, Vassilevski AA, Korolkova YV, Boychuk YA, Viatchenko-Karpinski VY, Nadezhdin KD, Arseniev AS, Pluzhnikov KA, Kulyk VB, Voitenko NV, Krishtal OO. Novel peptide from spider venom inhibits P2X3 receptors and inflammatory pain. Ann Neurol. 2010 May;67(5):680-3. PMID:20437566 doi:10.1002/ana.21949
  2. Kabanova NV, Vassilevski AA, Rogachevskaja OA, Bystrova MF, Korolkova YV, Pluzhnikov KA, Romanov RA, Grishin EV, Kolesnikov SS. Modulation of P2X3 receptors by spider toxins. Biochim Biophys Acta. 2012 Nov;1818(11):2868-75. doi: , 10.1016/j.bbamem.2012.07.016. Epub 2012 Jul 25. PMID:22842000 doi:http://dx.doi.org/10.1016/j.bbamem.2012.07.016
  3. Grishin EV, Savchenko GA, Vassilevski AA, Korolkova YV, Boychuk YA, Viatchenko-Karpinski VY, Nadezhdin KD, Arseniev AS, Pluzhnikov KA, Kulyk VB, Voitenko NV, Krishtal OO. Novel peptide from spider venom inhibits P2X3 receptors and inflammatory pain. Ann Neurol. 2010 May;67(5):680-3. PMID:20437566 doi:10.1002/ana.21949
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