Evidence 1
Activity
Activity
Neurotoxin
FUNCTION: Potent voltage-gated sodium channel blocker (By similarity). Potently inhibits the voltage-gated sodium channels Nav1.7/SCN9A (IC(50)=0.58-10 nM) (By similarity). 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) (By similarity) (PubMed:29703751). 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) (By similarity) (PubMed:29703751). Weakly blocks the low voltage-gated calcium channels Cav3.1/CACNA1G (30% inhibition of the peak current by 9.8 nM of the toxin) (PubMed:21740921). It shows moderate affinity for lipid bilayers (PubMed:29703751). {ECO:0000250|UniProtKB:P0DL72, ECO:0000250|UniProtKB:P0DL73, ECO:0000269|PubMed:21740921, ECO:0000269|PubMed:29703751}.
Target
voltage-gated sodium channel (Nav)
voltage-gated calcium channel (Cav)
Source & Reference
NA
UniProtKB/Swiss-Prot Tox-Prot
Other
Grammostola rosea (Chilean rose tarantula) (Grammostola spatulata)
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 (By similarity). Potently inhibits the voltage-gated sodium channels Nav1.7/SCN9A (IC(50)=0.58-10 nM) (By similarity).
Toxin GTx1-15 (Beta/omega-theraphotoxin-Gr2a) (Beta/omega-TRTX-Gr2a) (GpTx-1) (GpTx-I)
spider
Neurotoxin 10 (Hwtx-1) family, 08 (Gtx1-15) subfamily
Evidence at protein level
Amidation
Calcium channel impairing toxin
Direct protein sequencing
Disulfide bond
Ion channel impairing toxin
Knottin
Neurotoxin
Secreted
Signal
Toxin
Voltage-gated calcium channel impairing toxin
Voltage-gated sodium channel impairing toxin
TISSUE SPECIFICITY: Expressed by the venom gland. {ECO:0000305|PubMed:21740921}.