2kgu
From Proteopedia
Spatial structure of purotoxin-1 in water
Structural highlights
FunctionTXPR1_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 PubMedP2X3 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
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