Evidence 1
Activity
Activity
Neurotoxin
FUNCTION: Potent voltage-gated sodium channel blocker (PubMed:25658507). Potently inhibits the voltage-gated sodium channels Nav1.7/SCN9A (IC(50)=0.58-10 nM) (PubMed:25658507, PubMed:26999206). Also shows a moderate activity on Nav1.1/SCN1A (IC(50)=6 nM), Nav1.2/SCN2A (IC(50)=5-128 nM), Nav1.3/SCN3A (IC(50)=20.3-170 nM), and Nav1.6/SCN8A (IC(50)=17-20.1 nM) (PubMed:25658507, PubMed:26999206). Shows an unclear inhibition of Nav1.4/SCN4A (IC(50)=200 nM to >10 uM), Nav1.5/SCN5A (IC(50)=140 nM to >10 uM) and Nav1.8/SCN10A (IC(50)=68-12200 nM) (PubMed:25658507, PubMed:26999206). Weakly blocks the low voltage-gated calcium channels Cav3.1/CACNA1G (30% inhibition of the peak current at 9.8 nM) (By similarity). shows moderate affinity for lipid bilayers (By similarity). In vivo, when tested on the OD1-induced mouse model of Nav1.7/SCN9A-mediated pain, the toxin is effective when co-administered with OD1, but lacks efficacy when delivered systemically (PubMed:26999206). {ECO:0000250|UniProtKB:P0DJA9, ECO:0000250|UniProtKB:P0DL73, ECO:0000269|PubMed:25658507, ECO:0000269|PubMed:26999206}.
Target
voltage-gated sodium channel (Nav)
voltage-gated calcium channel (Cav)
Source & Reference
NA
UniProtKB/Swiss-Prot Tox-Prot
Other
Grammostola porteri (Tarantula spider) (Lasiodora porteri)
Neurotoxin
Calcium channel impairing toxin
Ion channel impairing toxin
Voltage-gated calcium channel impairing toxin
Voltage-gated sodium channel impairing toxin
Potent voltage-gated sodium channel blocker (PubMed:25658507). Potently inhibits the voltage-gated sodium channels Nav1.7/SCN9A (IC(50)=0.58-10 nM) (PubMed:25658507, PubMed:26999206).
Toxin GTx1-15 (Beta/omega-theraphotoxin-Gr2a) (Beta/omega-TRTX-Gr2a) (Toxin GpTx-1)
spider
Neurotoxin 10 (Hwtx-1) family, 08 (Gtx1-15) subfamily
Evidence at protein level
3D-structure
Amidation
Calcium channel impairing toxin
Direct protein sequencing
Disulfide bond
Ion channel impairing toxin
Knottin
Neurotoxin
Secreted
Toxin
Voltage-gated calcium channel impairing toxin
Voltage-gated sodium channel impairing toxin
TISSUE SPECIFICITY: Expressed by the venom gland. {ECO:0000305|PubMed:25658507}.