Evidence 1
Activity
Activity
Neurotoxin
FUNCTION: This gating-modifier toxin shows an important inhibitory activity on sodium channels (PubMed:29723257). It is very active on Nav1.7/SCN9A (IC(50)~0.6 nM), and also shows activity on Nav1.3/SCN3A (IC(50)=292 nM), Nav1.4/SCN4A (IC(50)=2.2-159 nM), and Nav1.5/SCN5A (IC(50)=2.3-2.9 uM) (PubMed:25055801, PubMed:29723257). It has also been shown to inhibit tetrodotoxin (TTX)-resistant (IC(50)=27.6 nM) and TTX-sensitive (IC(50)=30.2 nM) sodium channels in rat dorsal root ganglion neurons (PubMed:17157888). Lower inhibitory activity has also been shown on potassium channels: Kv4.2/KCND2 (IC(50)=604.2 nM), Kv4.3/KCND3 (IC(50)=425.1 nM), and Kv2.1/KCNB1 (IC(50)=14.3 uM) (PubMed:17150181, PubMed:17157888, PubMed:20571743). It binds to phospholipid membranes. Like its analog AM-8145, it may act by interacting only with the second voltage-sensor domain of Nav1.7/SCN9A (Probable). {ECO:0000269|PubMed:17150181, ECO:0000269|PubMed:17157888, ECO:0000269|PubMed:18581053, ECO:0000269|PubMed:20571743, ECO:0000269|PubMed:29723257}.
Target
voltage-gated sodium channel (Nav)
voltage-gated potassium channel (Kv)
Source & Reference
NA
UniProtKB/Swiss-Prot Tox-Prot
Other
Chilobrachys guangxiensis (Chinese earth tiger tarantula) (Chilobrachys jingzhao)
Neurotoxin
Ion channel impairing toxin
Potassium channel impairing toxin
Voltage-gated potassium channel impairing toxin
Voltage-gated sodium channel impairing toxin
This gating-modifier toxin shows an important inhibitory activity on sodium channels (PubMed:29723257). It is very active on Nav1.7/SCN9A (IC(50)~0.6 nM), and also shows activity on Nav1.3/SCN3A (IC(50)=292 nM), Nav1.4/SCN4A (IC(50)=2.2-159 nM), and Nav1.5/SCN5A (IC(50)=2.3-2.9 uM) (PubMed:25055801, PubMed:29723257).
Beta/kappa-theraphotoxin-Cg2a (Beta/kappa-TRTX-Cg2a) (Beta-theraphotoxin-Cj2a) (Jingzhaotoxin-5) (Jingzhaotoxin-V) (JZTX-V) (Peptide F8-15.73)
spider
Neurotoxin 30 (phrixotoxin) family
Evidence at protein level
3D-structure
Amidation
Direct protein sequencing
Disulfide bond
Ion channel impairing toxin
Knottin
Neurotoxin
Potassium channel impairing toxin
Secreted
Signal
Toxin
Voltage-gated potassium channel impairing toxin
Voltage-gated sodium channel impairing toxin
TISSUE SPECIFICITY: Expressed by the venom gland. {ECO:0000305|PubMed:17157888}.