Evidence 1
Activity
Activity
Neurotoxin
FUNCTION: Ion channel impairing toxin that inhibits voltage-gated calcium channel Cav3.1/CACNA1G (IC(50)=53 nM), voltage-gated potassium channels Kv2.1/KCNB1 (IC(50)=411 nM), all sodium channels tested (Nav1.2/SCN2A (IC(50)=60-104 nM), Nav1.5/SCN5A (IC(50)=76-358 nM), Nav1.6/SCN8A (IC(50)=21-133 nM), Nav1.7/SCN9A (IC(50)=51-95 nM), and Nav1.8/SCN10A) as well as the nociceptor cation channel TRPA1 (IC(50)=389 nM) (By similarity) (PubMed:32511987). Acts as a potent and selective blocker of voltage-gated calcium channel Cav3.1/CACNA1G, but not of Cav3.2/CACNA1H, and Cav3.3/CACNA1I (By similarity). On Nav1.7/SCN9A, primarily interacts with the DII and DIV voltage-sensor domains (PubMed:32511987). Also acts as an inhibitor of nociceptor cation channel TRPA1 (IC(50)~389 nM) by binding to the S1-S4 gating domain of TRPA1 (By similarity). It shows moderate affinity for lipid bilayers (By similarity). {ECO:0000250|UniProtKB:P83480, ECO:0000269|PubMed:32511987}.
Target
voltage-gated sodium channel (Nav)
voltage-gated potassium channel (Kv)
voltage-gated calcium channel (Cav)
TRP channel
Source & Reference
NA
UniProtKB/Swiss-Prot Tox-Prot
Other
Bumba pulcherrimaklaasi (Tarantula spider) (Euathlus pulcherrimaklaasi)
Neurotoxin
Calcium channel impairing toxin
Ion channel impairing toxin
Potassium channel impairing toxin
Voltage-gated calcium channel impairing toxin
Voltage-gated potassium channel impairing toxin
Voltage-gated sodium channel impairing toxin
Ion channel impairing toxin that inhibits voltage-gated calcium channel Cav3.1/CACNA1G (IC(50)=53 nM), voltage-gated potassium channels Kv2.1/KCNB1 (IC(50)=411 nM), all sodium channels tested (Nav1.2/SCN2A (IC(50)=60-104 nM), Nav1.5/SCN5A (IC(50)=76-358 nM), Nav1.6/SCN8A (IC(50)=21-133 nM), Nav1.7/SCN9A (IC(50)=51-95 nM), and Nav1.8/SCN10A) as well as the nociceptor cation channel TRPA1 (IC(50)=389 nM) (By similarity) (PubMed:32511987). Acts as a potent and selective blocker of voltage-gated calcium channel Cav3.1/CACNA1G, but not of Cav3.2/CACNA1H, and Cav3.3/CACNA1I (By similarity).
Beta/omega-theraphotoxin-Bp1a (Beta/omega-TRTX-Bp1a) (Protoxin-I analog) (ProTx-I analog)
spider
Neurotoxin 10 (Hwtx-1) family, 54 (ProTx-1) subfamily
Evidence at protein level
Calcium channel impairing toxin
Direct protein sequencing
Disulfide bond
Ion channel impairing toxin
Knottin
Neurotoxin
Pharmaceutical
Potassium channel impairing toxin
Secreted
Toxin
Voltage-gated calcium channel impairing toxin
Voltage-gated potassium channel impairing toxin
Voltage-gated sodium channel impairing toxin
TISSUE SPECIFICITY: Expressed by the venom gland. {ECO:0000305|PubMed:32511987}.