ProTx-III
ProTx-III (µ-TRTX-Tp1a; belongs to NaSpTx family 1) has been isolated from the venom of the Peruvian green-velvet tarantula Thrixopelma pruriens at the University of Queensland (Australia). ProTx-III has been described to be a selective inhibitor of Nav1.7 with an IC50 value around 2 nM. This synthetic version of Tp1a yields similar results in terms of Nav1.7 inhibition. Queensland scientists have described that ProTx-III induces no significant changes in the voltage dependence of activation or steady-state inactivation of Nav1.7. ProTx-III also inhibits Nav1.1, Nav1.2 and Nav1.6 at nanomolar concentrations and does not affects Cav channels and nicotinic acetylcholine receptors. ProTx-III demonstrates analgesic properties in vivo when injected intraplantary in mice prior treatment with OD1, an activator of Nav1.7, which induces spontaneous pain.
- Applications:Selective blocker of the sodium channel Nav1.7
Peptides & proteins
µ-TRTX-Tp1a
1) Fernanda C., et al. (2015) Identification and Characterization of ProTx-III [m-TRTX-Tp1a], a New Voltage-Gated Sodium Channel Inhibitor from Venom of the Tarantula Thrixopelma pruriens. PMID: 25979003.
RT
AA sequence: Asp-Cys2-Leu-Lys-Phe-Gly-Trp-Lys-Cys9-Asn-Pro-Arg-Asn-Asp-Lys-Cys16-Cys17-Ser-Gly-Leu-Lys-Cys22-Gly-Ser-Asn-His-Asn-Trp-Cys29-Lys-Leu-His-Ile-NH2; Disulfide bonds: Cys2-Cys17, Cys9-Cys22, Cys16-Cys29