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Peptide record

TPDB71953

Neurotoxin standard
57 amino acids
Basic Information
3D PDB MODEL
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TPDB71953
Neurotoxin
Toxicity and safety peptides
NTxPred2
standard
No
A 57-aa standard natural neurotoxin peptide sequence curated from NTxPred2, with an available 3D structural model.
Sequence
MKISFVLLLTLFICSIGWSEARPTDIKCSESYQCFPVCKSRFGKTNGRCVNGFCDCF
Physicochemical Analysis
C287H444N74O79S8
H
C
6451.61
8.19
7
4
21
+3
1.53
0.286
71.75
Mammalian: 30 hour Yeast: >20 hour E.coli: >10 hour
7365
114.16
20
Residue Composition
number
1
A
3
R
2
N
2
D
7
C
2
E
1
Q
4
G
0
H
4
I
4
L
4
K
1
M
6
F
2
P
6
S
3
T
1
W
1
Y
3
V
Amino Acid Distribution
A: 1 R: 3 N: 2 D: 2 C: 7 E: 2 Q: 1 G: 4 H: 0 I: 4 L: 4 K: 4 M: 1 F: 6 P: 2 S: 6 T: 3 W: 1 Y: 1 V: 3
Chemical Descriptors
57
C287H444N74O79S8
6451.61
8.19
+3
1.53
0.286
Evidence Records 1 records
Evidence 1 Activity

Activity

Neurotoxin
FUNCTION: Blocks human and/or rat Kv11.1/KCNH2/ERG1, Kv11.2/KCNH6/ERG2 and Kv11.3/KCNH7/ERG3 by binding to channel outer vestibule (S5P domain) with a 1:1 stoichiometry. Inhibition data are the following: hERG1 (reversible, Kd=7.7 nM (PubMed:16497878), IC(50)=3.3 nM (PubMed:11136720), IC(50)=11.9 nM (PubMed:21205913)), rERG1 (reversible, Kd=19 nM) (PubMed:16497878), hERG2 (reversible, Kd=77 nM) (PubMed:16497878), rERG2 (irreversible, Kd=4.2 nM) (PubMed:16497878), hERG3 (reversible, Kd=11.5 nM) (PubMed:16497878) and rERG3 (reversible, Kd=747 nM) (PubMed:16497878) potassium channels. Also has a minimal effect on rat ELK1/KCNH4 potassium channels (9% inhibition at 100 nM (PubMed:15137031)). Both this toxin and CnErgTx1 (AC Q86QT3) share mechanism of action and have overlapping binding sites on ERG1 (PubMed:12719233). The potency of these two toxins is not affected by elevating potassium ion concentration from 2 to 98 mM (PubMed:12719233). In addition, at high toxin concentrations, block of ERG1 macroscopic currents by these two toxins is incomplete (88%) (PubMed:12719233). The blockade by this toxin is preferentially closed channel state-dependent, with a component of open, but not inactive state-dependent blockade (PubMed:12860380). This toxin produces a concentration-dependent prolongation of QTc in the isolated rabbit heart (16.3% at 100 nM) (PubMed:21205913). {ECO:0000269|PubMed:11136720, ECO:0000269|PubMed:12719233, ECO:0000269|PubMed:12860380, ECO:0000269|PubMed:16497878, ECO:0000269|PubMed:21205913, ECO:0000269|PubMed:8617371}.

Target

voltage-gated potassium channel (Kv)

Source & Reference

NA
UniProtKB/Swiss-Prot Tox-Prot

Other

Mesobuthus eupeus (Lesser Asian scorpion) (Buthus eupeus)
Neurotoxin Ion channel impairing toxin Potassium channel impairing toxin Voltage-gated potassium channel impairing toxin
Blocks human and/or rat Kv11.1/KCNH2/ERG1, Kv11.2/KCNH6/ERG2 and Kv11.3/KCNH7/ERG3 by binding to channel outer vestibule (S5P domain) with a 1:1 stoichiometry. Inhibition data are the following: hERG1 (reversible, Kd=7.7 nM (PubMed:16497878), IC(50)=3.3 nM (PubMed:11136720), IC(50)=11.9 nM (PubMed:21205913)), rERG1 (reversible, Kd=19 nM) (PubMed:16497878), hERG2 (reversible, Kd=77 nM) (PubMed:16497878), rERG2 (irreversible, Kd=4.2 nM) (PubMed:16497878), hERG3 (reversible, Kd=11.5 nM) (PubMed:16497878) and rERG3 (reversible, Kd=747 nM) (PubMed:16497878) potassium channels.
Potassium channel toxin gamma-KTx 2.1 (Neurotoxin BeKm-1) (BeKm1)
scorpion
Short scorpion toxin superfamily, Potassium channel inhibitor family, Gamma-KTx 2 subfamily
Evidence at protein level
3D-structure Direct protein sequencing Disulfide bond Ion channel impairing toxin Neurotoxin Potassium channel impairing toxin Secreted Signal Toxin Voltage-gated potassium channel impairing toxin
TISSUE SPECIFICITY: Expressed by the venom gland. {ECO:0000305}.
Additional Detail Fields 7 fields
3D-structure Direct protein sequencing Disulfide bond Ion channel impairing toxin Neurotoxin Potassium channel impairing toxin Secreted Signal Toxin Voltage-gated potassium channel impairing toxin
Neurotoxin Ion channel impairing toxin Potassium channel impairing toxin Voltage-gated potassium channel impairing toxin
Evidence at protein level
Short scorpion toxin superfamily, Potassium channel inhibitor family, Gamma-KTx 2 subfamily
Potassium channel toxin gamma-KTx 2.1 (Neurotoxin BeKm-1) (BeKm1)
TISSUE SPECIFICITY: Expressed by the venom gland. {ECO:0000305}.
scorpion