General Information of This Peptide
Peptide ID
BTDP008536
Peptide Name
Potassium channel toxin gamma-KTx 2.1
Symonym
Neurotoxin BeKm-1
Species
Mesobuthus eupeus (Lesser Asian scorpion) (Buthus eupeus)
Uniprot Name
KGX21_MESEU
Alphafold ID
Q9BKB7
3D Structure
Download
2D Sequence
3D Structure
Source
RSCB PDB: 1J5J
Sequence
MKISFVLLLTLFICSIGWSEARPTDIKCSESYQCFPVCKSRFGKTNGRCVNGFCDCF
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Sequence Length
57
Mass (Da)
6452
Signal Sequence
MKISFVLLLTLFICSIGWSEA
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Sequence Removed Signal Peptide
RPTDIKCSESYQCFPVCKSRFGKTNGRCVNGFCDCF
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Disulfide Bond
28-49;34-54;38-56
PDB ID
1J5J , 1LGL
        Click to Show/Hide the Complete Species Lineage
Kingdom: Metazoa
Phylum: Arthropoda
Class: Arachnida
Order: Scorpiones
Family: Buthidae
Genus: Mesobuthus
Species: Mesobuthus eupeus
Full List of Activity Data of This Peptide Toxin
                        Target Name Activity Data Type Activity Data Concentration Note Reference
 Target Info    Kv11.2 Dissociation constant
4.2 nM
.
Irreversible
[1- 10]
 Target Info    Kv11.2 Dissociation constant
4.2 nM
.
Blocker
[1- 10]
 Target Info    Kv11 Dissociation constant
7.7 nM
.
Blocker
[6]
 Target Info    Kv11/ERG Dissociation constant
7.7 nM
.
Reversible
[1- 10]
 Target Info    Kv11.3 Dissociation constant
11.5 nM
.
Reversible
[1- 10]
 Target Info    Kv11.3 Dissociation constant
11.5 nM
.
Blocker
[6]
 Target Info    Kv11.1 Dissociation constant
19 nM
.
Reversible
[1- 10]
 Target Info    Kv11.1 Dissociation constant
19 nM
.
Blocker
[1- 10]
 Target Info    ERG2 Dissociation constant
77 nM
.
Reversible
[1- 10]
 Target Info    Kv11.2 Dissociation constant
77 nM
.
Blocker
[6]
 Target Info    Kv11.3 Dissociation constant
747 nM
.
Reversible
[1- 10]
 Target Info    Kv11.3 Dissociation constant
747 nM
.
Blocker
[1- 10]
 Target Info    Kir1.1 Inhibition rate .
50 nM
Block macroscopic current
[1- 10]
 Target Info    KCa3.1 Inhibition rate .
100 nM
Block macroscopic current
[1- 10]
 Target Info    Kir1.1 Inhibition rate .
100 nM
Blocker
[1- 10]
 Target Info    Kv1.2 Inhibition rate .
50 nM
Block macroscopic current
[1- 10]
 Target Info    KCa3.1 Inhibition rate .
100 nM
Blocker
[1]
 Target Info    Kv7.2 Inhibition rate .
100 nM
Blocker
[1]
 Target Info    EAG1 Inhibition rate .
100 nM
Block macroscopic current
[1- 10]
 Target Info    Kv1.2 Inhibition rate .
50 nM
Blocker
[1- 10]
 Target Info    Kv7.1 Inhibition rate .
100 nM
Blocker
[1]
 Target Info    Kv7.4 Inhibition rate .
100 nM
Blocker
[1]
 Target Info    Kv1.4 Inhibition rate .
50 nM
Block macroscopic current
[1- 10]
 Target Info    Kv1.4 Inhibition rate .
50 nM
Blocker
[1- 10]
 Target Info    KCa2 Inhibition rate .
100 nM
Block macroscopic current
[1- 10]
 Target Info    KCa2 Inhibition rate .
100 nM
Blocker
[1]
 Target Info    Kv10 Inhibition rate .
100 nM
Blocker
[1]
 Target Info    Kv2.1 Inhibition rate .
50 nM
Block macroscopic current
[1- 10]
 Target Info    Kv2.1 Inhibition rate .
50 nM
Blocker
[1- 10]
 Target Info    Kv4.3 Inhibition rate .
50 nM
Block macroscopic current
[1- 10]
 Target Info    Kv4.3 Inhibition rate .
50 nM
Blocker
[1- 10]
 Target Info    KCa1.1 Inhibition rate .
100 nM
Block macroscopic current
[1- 10]
 Target Info    KCa2.1 Inhibition rate .
100 nM
Blocker
[1]
 Target Info    KCNQ1 and KCNE1 Inhibition rate .
100 nM
Block macroscopic current
[1- 10]
 Target Info    Kv7.2/7.3 Inhibition rate .
100 nM
Block macroscopic current
[1- 10]
 Target Info    Kv7.4 Inhibition rate .
100 nM
Block macroscopic current
[1- 10]
 Target Info    KCa2.1 Inhibition rate .
100 nM
Block macroscopic current
[1- 10]
 Target Info    KCa1.1 Inhibition rate .
100 nM
Blocker
[1]
 Target Info    Kv2.3 Inhibition rate .
100 nM
Blocker
[1]
 Target Info    ELK1 Inhibition rate
9 %
100 nM
Block macroscopic current
[1- 10]
 Target Info    Kv12.1 Inhibition rate
10 %
100 nM
Blocker
[1]
 Target Info    ERG1 Inhibition rate
88 %
.
Block macroscopic current
[1- 10]
 Target Info    Kv11/ERG IC50
3.3 nM
.
Reversible
[1- 10]
 Target Info    ERG1 IC50
7.6 nM
.
At room temperature
[1- 10]
 Target Info    Kv11 IC50
7.7 nM
.
Blocker
[1]
 Target Info    Kv11/ERG IC50
11.9 nM
.
Reversible
[1- 10]
 Target Info    ERG1 IC50
15.3 nM
.
At 37°C
[1- 10]
References
Ref 1 An ERG channel inhibitor from the scorpion Buthus eupeus. J Biol Chem. 2001 Mar 30;276(13):9868-76. doi: 10.1074/jbc.M005973200. Epub 2001 Jan 2.
Ref 2 M-type K+ current inhibition by a toxin fron the scorpion Buthus eupeus. FEBS Lett. 1996 Apr 22;384(3):277-80. doi: 10.1016/0014-5793(96)00333-x.
Ref 3 BeKm-1 is a HERG-specific toxin that shares the structure with ChTx but the mechanism of action with ErgTx1. Biophys J. 2003 May;84(5):3022-36. doi: 10.1016/S0006-3495(03)70028-9.
Ref 4 Preferential closed channel blockade of HERG potassium currents by chemically synthesised BeKm-1 scorpion toxin. FEBS Lett. 2003 Jul 17;547(1-3):20-6. doi: 10.1016/s0014-5793(03)00662-8.
Ref 5 Unique interaction of scorpion toxins with the hERG channel. J Mol Recognit. 2004 May-Jun;17(3):209-17. doi: 10.1002/jmr.667.
Ref 6 Species diversity and peptide toxins blocking selectivity of ether-a-go-go-related gene subfamily K+ channels in the central nervous system. Mol Pharmacol. 2006 May;69(5):1673-83. doi: 10.1124/mol.105.019729. Epub 2006 Feb 23.
Ref 7 BeKm-1, a peptide inhibitor of human ether-a-go-go-related gene potassium currents, prolongs QTc intervals in isolated rabbit heart. J Pharmacol Exp Ther. 2011 Apr;337(1):2-8. doi: 10.1124/jpet.110.176883. Epub 2010 Dec 23.
Ref 8 A large number of novel Ergtoxin-like genes and ERG K+-channels blocking peptides from scorpions of the genus Centruroides. FEBS Lett. 2002 Dec 4;532(1-2):121-6. doi: 10.1016/s0014-5793(02)03652-9.
Ref 9 Interaction simulation of hERG K+ channel with its specific BeKm-1 peptide: insights into the selectivity of molecular recognition. J Proteome Res. 2007 Feb;6(2):611-20. doi: 10.1021/pr060368g.
Ref 10 New binding site on common molecular scaffold provides HERG channel specificity of scorpion toxin BeKm-1. J Biol Chem. 2002 Nov 8;277(45):43104-9. doi: 10.1074/jbc.M204083200. Epub 2002 Jul 31.
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