Novel peptide from spider venom inhibits P2X3 receptors and inflammatory pain.
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.
Grishin
Eugene V
EV
Laboratory of Neuroreceptors and Neuroregulators, Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Moscow, Russia.
Savchenko
Ganna A
GA
Vassilevski
Alexander A
AA
Korolkova
Yuliya V
YV
Boychuk
Yaroslav A
YA
Viatchenko-Karpinski
Viacheslav Y
VY
Nadezhdin
Kirill D
KD
Arseniev
Alexander S
AS
Pluzhnikov
Kirill A
KA
Kulyk
Vyacheslav B
VB
Voitenko
Nana V
NV
Krishtal
Oleg O
OO
D000255:Adenosine Triphosphate / Q000494:pharmacology; D000818:Animals; D000831:Animals, Newborn; D002478:Cells, Cultured; D044723:Chondrus; D003570:Cytidine Triphosphate / Q000494:pharmacology; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D005727:Ganglia, Spinal / Q000166:cytology; D006801:Humans; D009682:Magnetic Resonance Spectroscopy / Q000379:methods; D008564:Membrane Potentials / Q000187:drug effects / Q000235:genetics; D020078:Neurogenic Inflammation / Q000139:chemically induced / Q000150:complications; D010146:Pain / Q000188:drug therapy* / Q000209:etiology / Q000378:metabolism*; D018408:Patch-Clamp Techniques / Q000379:methods; D010455:Peptides / Q000627:therapeutic use*; D058919:Purinergic P2 Receptor Antagonists; D051381:Rats; D017208:Rats, Wistar; D018048:Receptors, Purinergic P2 / Q000235:genetics / Q000378:metabolism*; D058477:Receptors, Purinergic P2X3; D011984:Sensory Receptor Cells / Q000187:drug effects / Q000502:physiology; D013111:Spider Venoms / Q000737:chemistry*; D014162:Transfection / Q000379:methods
C546407:P2RX3 protein, human; D010455:Peptides; D058919:Purinergic P2 Receptor Antagonists; D018048:Receptors, Purinergic P2; D058477:Receptors, Purinergic P2X3; D013111:Spider Venoms; C549443:purotoxin-1, Geolycosa; D003570:Cytidine Triphosphate; D000255:Adenosine Triphosphate