Glycyl-poneratoxin

UniProtKB accession:  P41736

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UniProtKB description:  Toxin that causes pain in vertebrates by targeting tetrodotoxin (TTX)-sensitive sodium channels in peripheral sensory neurons (PubMed:37221205). Also blocks synaptic transmission and stimulates smooth muscle contraction (PubMed:12097919, PubMed:1685424, PubMed:1685425). Converts the normally rapidly activating and inactivating sodium channel current into one that does not inactivate (PubMed:27266841, PubMed:37221205). Is active on both Nav1.6/SCN8A and Nav1.7/SCN9A sodium channels, with a much potent activity on Nav1.6/SCN8A (EC(50)=97 nM on human channels) than on Nav1.7/SCN9A (EC(50)=2.3 uM on human and EC(50)=1.8 uM on mouse channels) (PubMed:27266841, PubMed:37221205). On these channels, causes a sustained current, a reduction in peak current amplitude and a hyperpolarising shift (PubMed:27266841, PubMed:37221205). Modulates Nav1.7/SCN9A in a non-competitive manner with TTX or tetracaine (Probable). Toxin-induced persistant current is very slowly reversible with repeated wash steps over 30 minutes (PubMed:37221205). In vivo, shallow intraplantar injection in mice causes immediate, long-lasting and near-maximal nocifensive behaviors, which decrease with coinjection of TTX (PubMed:37221205). When tested on insects, causes paralysis but not mortality at high doses (PubMed:37221205).