Evidence 1
Activity
Activity
Neurotoxin
FUNCTION: Potently and reversibly inhibits some human voltage-gated sodium channels (Nav1.1/SCN1A (IC(50)=72.0 nM), Nav1.2/SCN2A (IC(50)=75.5 nM), Nav1.6/SCN8A (IC(50)=115.0 nM), Nav1.7/SCN9A (IC(50)=52.7-129.5 nM), Nav1.3/SCN3A (IC(50)=306.6 nM)) (PubMed:30784059). The hNav1.7/SCN9A channel inhibition occurs without any change in steady-state inactivation- and conductance-voltage relationships (PubMed:30784059). On adult mouse DRG neurons, this toxin is approximately 1000-fold more efficient to inhibit tetrodotoxin (TTX)-sensitive than TTX-resistant sodium currents (PubMed:30784059). In vivo, this toxin exhibits analgesic effects in mice pain models (PubMed:30784059). {ECO:0000269|PubMed:30784059}.
Target
voltage-gated sodium channel (Nav)
Source & Reference
NA
UniProtKB/Swiss-Prot Tox-Prot
Other
Omothymus schioedtei (Malaysian earth tiger tarantula) (Cyriopagopus schioedtei)
Neurotoxin
Ion channel impairing toxin
Voltage-gated sodium channel impairing toxin
Potently and reversibly inhibits some human voltage-gated sodium channels (Nav1.1/SCN1A (IC(50)=72.0 nM), Nav1.2/SCN2A (IC(50)=75.5 nM), Nav1.6/SCN8A (IC(50)=115.0 nM), Nav1.7/SCN9A (IC(50)=52.7-129.5 nM), Nav1.3/SCN3A (IC(50)=306.6 nM)) (PubMed:30784059). The hNav1.7/SCN9A channel inhibition occurs without any change in steady-state inactivation- and conductance-voltage relationships (PubMed:30784059).
Mu-theraphotoxin-Os1a (Mu-TRTX-Os1a) (Cyriotoxin-1a) (CyrTx-1a) (Mu-theraphotoxin-Cs1a)
spider
Neurotoxin 10 (Hwtx-1) family, 14 (Hntx-1) subfamily
Evidence at protein level
3D-structure
Amidation
Direct protein sequencing
Disulfide bond
Ion channel impairing toxin
Neurotoxin
Secreted
Toxin
Voltage-gated sodium channel impairing toxin
TISSUE SPECIFICITY: Expressed by the venom gland. {ECO:0000305|PubMed:30784059}.