General Information of This Peptide
Peptide ID
BTDP008444
Peptide Name
Potassium channel toxin alpha-KTx 1.1
Symonym
ChTX-Lq1; ChTx-a; Charybdotoxin
Species
Leiurus hebraeus (Deathstalker scorpion) (Leiurus quinquestriatus hebraeus)
Uniprot Name
KAX11_LEIHE
Alphafold ID
P13487
3D Structure
Download
2D Sequence
3D Structure
Source
RSCB PDB: 1BAH
Sequence
MKILSVLLLALIICSIVGWSEAQFTNVSCTTSKECWSVCQRLHNTSRGKCMNKKCRCYS
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Sequence Length
59
Mass (Da)
6674
Signal Sequence
MKILSVLLLALIICSIVGWSEA
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Sequence Removed Signal Peptide
QFTNVSCTTSKECWSVCQRLHNTSRGKCMNKKCRCYS
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Disulfide Bond
29-50;35-55;39-57
PDB ID
1BAH , 1CMR , 2A9H , 2CRD , 4JTA , 4JTC , 4JTD
        Click to Show/Hide the Complete Species Lineage
Kingdom: Metazoa
Phylum: Arthropoda
Class: Arachnida
Order: Scorpiones
Family: Buthidae
Genus: Leiurus
Species: Leiurus quinquestriatus
Full List of Activity Data of This Peptide Toxin
                        Target Name Activity Data Type Activity Data Concentration Note Reference
 Target Info    Kv1.5 Dissociation constant
>100 nM
.
Blocker
[1- 21]
 Target Info    Kv1.3 Dissociation constant
2 nM
.
Blocker
[22]
 Target Info    KCa1.1 Dissociation constant
3.5 nM
.
Blocker
[12]
 Target Info    KCa3.1 Dissociation constant
5 nM
.
Blocker
[22]
 Target Info    KCa3.1 Dissociation constant
5 nM
.
Blocker
[23- 34]
 Target Info    KCa1.1 Dissociation constant
5 nM
.
Blocker
[22]
 Target Info    Kv1.2 Dissociation constant
9 nM
.
Blocker
[1- 21]
 Target Info    Kv1.2 Dissociation constant
10 nM
.
Blocker
[1- 21]
 Target Info    Kv3.1 Dissociation constant
>1 μM
.
Blocker
[1- 21]
 Target Info    Kv1.3 Inhibition constant
0.19 nM
.
Blocker
[1- 21]
 Target Info    Kv1.2-1.1 Inhibition constant
0.318 nM
.
Blocker
[35]
 Target Info    Kv1.6 Inhibition constant
22 nM
.
Blocker
[1- 21]
 Target Info    Kv1.6 Inhibition constant
22 nM
.
Blocker
[1- 21]
 Target Info    Shaker-IR Inhibition constant
227 nM
.
Blocker
[1- 21]
 Target Info    Shaker Inhibition constant
227 nM
.
Blocker
[7]
 Target Info    Kv2.1 Inhibition constant
>2 μM
.
Blocker
[1- 21]
 Target Info    Kv1 Inhibition constant
1.5 μM
.
Blocker
[1- 21]
 Target Info    Kv2.1 Inhibition rate .
2 μM
Blocker
[7]
 Target Info    Kir3.1/3.4 Inhibition rate .
1 μM
Blocker
[36]
 Target Info    Kir1.1 Inhibition rate
10 %
2.5 μM
Blocker
[37]
 Target Info    KCa1.1 IC50
5.9 nM
.
Blocker
[1- 21]
 Target Info    KCa2.1 IC50
>1 μM
.
Blocker
[1- 21]
 Target Info    KCa2.2 IC50
>1 μM
.
Blocker
[1- 21]
 Target Info    KCa2.3 IC50
>1 μM
.
Blocker
[1- 21]
References
Ref 1 Dynamic diversification from a putative common ancestor of scorpion toxins affecting sodium, potassium, and chloride channels. J Mol Evol. 1999 Feb;48(2):187-96. doi: 10.1007/pl00006457.
Ref 2 Purification, sequence, and model structure of charybdotoxin, a potent selective inhibitor of calcium-activated potassium channels. Proc Natl Acad Sci U S A. 1988 May;85(10):3329-33. doi: 10.1073/pnas.85.10.3329.
Ref 3 Charybdotoxin is a new member of the K+ channel toxin family that includes dendrotoxin I and mast cell degranulating peptide. Biochemistry. 1989 Dec 12;28(25):9708-14. doi: 10.1021/bi00451a025.
Ref 4 Analysis of the blocking activity of charybdotoxin homologs and iodinated derivatives against Ca2+-activated K+ channels. J Membr Biol. 1989 Aug;109(3):269-81. doi: 10.1007/BF01870284.
Ref 5 Solution synthesis of charybdotoxin (ChTX), a K+ channel blocker. Biochem Biophys Res Commun. 1990 Jul 31;170(2):684-90. doi: 10.1016/0006-291x(90)92145-p.
Ref 6 Synthesis and structural characterization of charybdotoxin, a potent peptidyl inhibitor of the high conductance Ca2(+)-activated K+ channel. J Biol Chem. 1990 Nov 5;265(31):18745-8.
Ref 7 Purification and characterization of three inhibitors of voltage-dependent K+ channels from Leiurus quinquestriatus var. hebraeus venom. Biochemistry. 1994 Jun 7;33(22):6834-9. doi: 10.1021/bi00188a012.
Ref 8 Pharmacological characterization of five cloned voltage-gated K+ channels, types Kv1.1, 1.2, 1.3, 1.5, and 3.1, stably expressed in mammalian cell lines. Mol Pharmacol. 1994 Jun;45(6):1227-34.
Ref 9 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 10 Maurotoxin: a potent inhibitor of intermediate conductance Ca2+-activated potassium channels. Mol Pharmacol. 2003 Feb;63(2):409-18. doi: 10.1124/mol.63.2.409.
Ref 11 Multidimensional signatures in antimicrobial peptides. Proc Natl Acad Sci U S A. 2004 May 11;101(19):7363-8. doi: 10.1073/pnas.0401567101. Epub 2004 Apr 26.
Ref 12 A designer ligand specific for Kv1.3 channels from a scorpion neurotoxin-based library. Proc Natl Acad Sci U S A. 2009 Dec 29;106(52):22211-6. doi: 10.1073/pnas.0910123106. Epub 2009 Dec 10.
Ref 13 Scorpion Potassium Channel-blocking Defensin Highlights a Functional Link with Neurotoxin. J Biol Chem. 2016 Mar 25;291(13):7097-106. doi: 10.1074/jbc.M115.680611. Epub 2016 Jan 27.
Ref 14 Scorpion toxins interact with nicotinic acetylcholine receptors. FEBS Lett. 2019 Oct;593(19):2779-2789. doi: 10.1002/1873-3468.13530. Epub 2019 Jul 18.
Ref 15 Molecular structure of charybdotoxin, a pore-directed inhibitor of potassium ion channels. Science. 1990 Aug 3;249(4968):521-4. doi: 10.1126/science.1696395.
Ref 16 Molecular structure of charybdotoxin: retraction. Science. 1991 May 3;252(5006):631. doi: 10.1126/science.252.5006.631.b.
Ref 17 Three-dimensional structure of natural charybdotoxin in aqueous solution by 1H-NMR. Charybdotoxin possesses a structural motif found in other scorpion toxins. Eur J Biochem. 1991 Feb 26;196(1):19-28. doi: 10.1111/j.1432-1033.1991.tb15780.x.
Ref 18 Refined structure of charybdotoxin: common motifs in scorpion toxins and insect defensins. Science. 1991 Dec 6;254(5037):1521-3. doi: 10.1126/science.1720574.
Ref 19 Analysis of side-chain organization on a refined model of charybdotoxin: structural and functional implications. Biochemistry. 1992 Sep 1;31(34):7756-64. doi: 10.1021/bi00149a003.
Ref 20 Progress in multidimensional NMR investigations of peptide and protein 3-D structures in solution. From structure to functional aspects. Biochimie. 1992 Sep-Oct;74(9-10):825-36. doi: 10.1016/0300-9084(92)90065-m.
Ref 21 NMR solution structure of a two-disulfide derivative of charybdotoxin: structural evidence for conservation of scorpion toxin alpha/beta motif and its hydrophobic side chain packing. Biochemistry. 1997 Apr 1;36(13):3760-6. doi: 10.1021/bi962720h.
Ref 22 Structure-guided transformation of charybdotoxin yields an analog that selectively targets Ca(2+)-activated over voltage-gated K(+) channels. J Biol Chem. 2000 Jan 14;275(2):1201-8. doi: 10.1074/jbc.275.2.1201.
Ref 23 Synthesis of Novel cis-2-Azetidinones from imines and aclychloride using triethylamine. Acta Chim Slov. 2023 Dec 4;70(4):628-633. doi: 10.17344/acsi.2023.8451.
Ref 24 Backward-Eulerian Footprint Modelling Based on the Adjoint Equation for Atmospheric and Urban-Terrain Dispersion. Boundary Layer Meteorol. 2023;188(1):159-183. doi: 10.1007/s10546-023-00807-z. Epub 2023 Apr 17.
Ref 25 Leaf spot on Alocasia macrorrhizos caused by Fusarium asiaticum in Sichuan, China. Plant Dis. 2022 Sep 11. doi: 10.1094/PDIS-04-22-0844-PDN. Online ahead of print.
Ref 26 Incidence and predictors of chronic kidney disease in type-II diabetes mellitus patients attending at the Amhara region referral hospitals, Ethiopia: A follow-up study. PLoS One. 2022 Jan 26;17(1):e0263138. doi: 10.1371/journal.pone.0263138. eCollection 2022.
Ref 27 A Method for More Accurate Determination of Resonance Frequency of the Cardiovascular System, and Evaluation of a Program to Perform It. Appl Psychophysiol Biofeedback. 2022 Mar;47(1):17-26. doi: 10.1007/s10484-021-09524-0. Epub 2021 Oct 16.
Ref 28 First Report of Fusarium wilt of Coleus forskohlii Caused by Fusarium oxysporum in China. Plant Dis. 2021 Jan 26. doi: 10.1094/PDIS-11-20-2489-PDN. Online ahead of print.
Ref 29 Shock waves from the inhomogeneous Boltzmann equation. Phys Rev E. 2019 Dec;100(6-1):062120. doi: 10.1103/PhysRevE.100.062120.
Ref 30 Classifying Changes to Preventive Interventions: Applying Adaptation Taxonomies. J Prim Prev. 2019 Feb;40(1):89-109. doi: 10.1007/s10935-018-00531-2.
Ref 31 Quantification of the passive and active biaxial mechanical behaviour and microstructural organization of rat thoracic ducts. J R Soc Interface. 2015 Jul 6;12(108):20150280. doi: 10.1098/rsif.2015.0280.
Ref 32 A model of mechanical interactions between heart and lungs. Philos Trans A Math Phys Eng Sci. 2009 Dec 13;367(1908):4741-57. doi: 10.1098/rsta.2009.0137.
Ref 33 Experimental test of nonlocal realistic theories without the rotational symmetry assumption. Phys Rev Lett. 2007 Nov 23;99(21):210406. doi: 10.1103/PhysRevLett.99.210406. Epub 2007 Nov 21.
Ref 34 Structures and phase transitions of the A7PSe6 (A = ag, Cu) argyrodite-type ionic conductors. III. alpha-Cu7PSe6. Acta Crystallogr B. 2000 Dec;56 (Pt 6):972-9. doi: 10.1107/s0108768100010260.
Ref 35 Characterization of a novel radiolabeled peptide selective for a subpopulation of voltage-gated potassium channels in mammalian brain. J Biol Chem. 2002 Feb 8;277(6):3886-93. doi: 10.1074/jbc.M109886200. Epub 2001 Nov 13.
Ref 36 A novel high-affinity inhibitor for inward-rectifier K+ channels. Biochemistry. 1998 Sep 22;37(38):13291-9. doi: 10.1021/bi981178p.
Ref 37 Purification, characterization, and synthesis of an inward-rectifier K+ channel inhibitor from scorpion venom. Biochemistry. 1997 Jun 10;36(23):6936-40. doi: 10.1021/bi9702849.
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