Peptide Information

General Information of This Peptide
Peptide ID
BTDP008391
Peptide Name
Kappa-stichotoxin-She3a
Symonym
Potassium channel toxin ShK
Species
Stichodactyla helianthus (Sun anemone) (Stoichactis helianthus)
Uniprot Name
K1A_STIHL
Alphafold ID
P29187
3D Structure
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2D Sequence
3D Structure
Source
RSCB PDB: 1BEI
Sequence
RSCIDTIPKSRCTAFQCKHSMKYRLSFCRKTCGTC
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Sequence Length
35
Mass (Da)
4061
Sequence Removed Signal Peptide
RSCIDTIPKSRCTAFQCKHSMKYRLSFCRKTCGTC
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Disulfide Bond
3-35;12-28;17-32
PDB ID
1BEI , 1C2U , 1ROO , 2K9E , 4LFQ , 4LFS , 4Z7P , 5I5A , 5I5B , 5I5C
        Click to Show/Hide the Complete Species Lineage
Kingdom: Metazoa
Phylum: Cnidaria
Class: Anthozoa
Order: Actiniaria
Family: Stichodactylidae
Genus: Stichodactyla
Species: Stichodactyla helianthus
Full List of Activity Data of This Peptide Toxin
                        Target Name Activity Data Type Activity Data Concentration Note Reference
 Target Info    KCa3.1 Dissociation constant
0.03 - 30 nM
 .
Blocker
 [1- 16]
 Target Info    KCa3.1 Dissociation constant
172 nM
 .
Blocker
 [4]
 Target Info    Kv1.2-1.1 Inhibition constant
0.03 nM
 .
Blocker
 [17]
 Target Info    Kv1.2-1.1 Inhibition constant
0.08 nM
 .
Blocker
 [17]
 Target Info    Shaker Inhibition constant
2 nM
 .
Blocker
 [18]
 Target Info    Shaker-KcsA Inhibition constant
50 nM
 .
Blocker
 [18]
 Target Info    Kv3.1 Inhibition rate .
100 nM
Blocker
 [11]
 Target Info    Kv1.5 Inhibition rate .
100 nM
Blocker
 [11]
 Target Info    Kv3.4 Inhibition rate .
100 nM
Blocker
 [11]
 Target Info    Kv2.1 Inhibition rate .
1 μM
Blocker
 [19]
 Target Info    Kir3.1/3.4 Inhibition rate .
1 μM
Blocker
 [1- 16]
 Target Info    Kv1.1 IC50
6.7 - 87 pM
 .
Blocker
 [1- 16]
 Target Info    Kv1.3 IC50
10 - 250 pM
 .
Blocker
 [1- 16]
 Target Info    Kv1.3 IC50
0.011 nM
 .
Blocker
 [11]
 Target Info    Kv1.1 IC50
0.016 nM
 .
Blocker
 [11]
 Target Info    Kv1 IC50
0.02 nM
 .
Blocker
 [1- 16]
 Target Info    Kv1.6 IC50
0.16 nM
 .
Blocker
 [1- 16]
 Target Info    Kv1.6 IC50
0.165 nM
 .
Blocker
 [11]
 Target Info    Kv1.4 IC50
0.31 nM
 .
Blocker
 [1- 16]
 Target Info    Kv1.4 IC50
0.312 nM
 .
Blocker
 [11]
 Target Info    Kv3.2 IC50
6 nM
 .
Blocker
 [19]
 Target Info    Kv1.2 IC50
9 nM
 .
Blocker
 [1- 16]
 Target Info    Kv1.2 IC50
9 nM
 .
Blocker
 [1- 16]
 Target Info    Kv1.7 IC50
11.5 nM
 .
Blocker
 [11]
 Target Info    Kv1.7 IC50
11.5 nM
 .
Blocker
 [1- 16]
 Target Info    KCa3.1 IC50
28 nM
 .
Blocker
 [11]
References
Ref 1 Characterization of a potassium channel toxin from the Caribbean Sea anemone Stichodactyla helianthus. Toxicon. 1995 May;33(5):603-13. doi: 10.1016/0041-0101(95)00013-c.
Ref 2 Chemical synthesis and characterization of ShK toxin: a potent potassium channel inhibitor from a sea anemone. Int J Pept Protein Res. 1995 Nov;46(5):354-8. doi: 10.1111/j.1399-3011.1995.tb01068.x.
Ref 3 Identification of three separate binding sites on SHK toxin, a potent inhibitor of voltage-dependent potassium channels in human T-lymphocytes and rat brain. Biochem Biophys Res Commun. 1996 Feb 27;219(3):696-701. doi: 10.1006/bbrc.1996.0297.
Ref 4 Structural conservation of the pores of calcium-activated and voltage-gated potassium channels determined by a sea anemone toxin. J Biol Chem. 1999 Jul 30;274(31):21885-92. doi: 10.1074/jbc.274.31.21885.
Ref 5 Targeting effector memory T cells with a selective peptide inhibitor of Kv1.3 channels for therapy of autoimmune diseases. Mol Pharmacol. 2005 Apr;67(4):1369-81. doi: 10.1124/mol.104.008193. Epub 2005 Jan 21.
Ref 6 Development of a rational nomenclature for naming peptide and protein toxins from sea anemones. Toxicon. 2012 Sep 15;60(4):539-50. doi: 10.1016/j.toxicon.2012.05.020. Epub 2012 Jun 5.
Ref 7 Defensin-neurotoxin dyad in a basally branching metazoan sea anemone. FEBS J. 2017 Oct;284(19):3320-3338. doi: 10.1111/febs.14194. Epub 2017 Sep 6.
Ref 8 Development of a sea anemone toxin as an immunomodulator for therapy of autoimmune diseases. Toxicon. 2012 Mar 15;59(4):529-46. doi: 10.1016/j.toxicon.2011.07.016. Epub 2011 Aug 12.
Ref 9 Sea Anemones: Quiet Achievers in the Field of Peptide Toxins. Toxins (Basel). 2018 Jan 8;10(1):36. doi: 10.3390/toxins10010036.
Ref 10 Solution structure of ShK toxin, a novel potassium channel inhibitor from a sea anemone. Nat Struct Biol. 1996 Apr;3(4):317-20. doi: 10.1038/nsb0496-317.
Ref 11 ShK-Dap22, a potent Kv1.3-specific immunosuppressive polypeptide. J Biol Chem. 1998 Dec 4;273(49):32697-707. doi: 10.1074/jbc.273.49.32697.
Ref 12 Role of disulfide bonds in the structure and potassium channel blocking activity of ShK toxin. Biochemistry. 1999 Nov 2;38(44):14549-58. doi: 10.1021/bi991282m.
Ref 13 Engineering a stable and selective peptide blocker of the Kv1.3 channel in T lymphocytes. Mol Pharmacol. 2009 Apr;75(4):762-73. doi: 10.1124/mol.108.052704. Epub 2009 Jan 2.
Ref 14 Native chemical ligation at Asx-Cys, Glx-Cys: chemical synthesis and high-resolution X-ray structure of ShK toxin by racemic protein crystallography. J Am Chem Soc. 2013 Aug 14;135(32):11911-9. doi: 10.1021/ja4046795. Epub 2013 Aug 6.
Ref 15 Pharmaceutical Optimization of Peptide Toxins for Ion Channel Targets: Potent, Selective, and Long-Lived Antagonists of Kv1.3. J Med Chem. 2015 Sep 10;58(17):6784-802. doi: 10.1021/acs.jmedchem.5b00495. Epub 2015 Aug 31.
Ref 16 Inversion of the Side-Chain Stereochemistry of Indvidual Thr or Ile Residues in a Protein Molecule: Impact on the Folding, Stability, and Structure of the ShK Toxin. Angew Chem Int Ed Engl. 2017 Mar 13;56(12):3324-3328. doi: 10.1002/anie.201612398. Epub 2017 Feb 14.
Ref 17 Substitution of a single residue in Stichodactyla helianthus peptide, ShK-Dap22, reveals a novel pharmacological profile. Biochemistry. 2003 Nov 25;42(46):13698-707. doi: 10.1021/bi035209e.
Ref 18 Designer and natural peptide toxin blockers of the KcsA potassium channel identified by phage display. Proc Natl Acad Sci U S A. 2015 Dec 15;112(50):E7013-21. doi: 10.1073/pnas.1514728112. Epub 2015 Dec 1.
Ref 19 Stichodactyla helianthus peptide, a pharmacological tool for studying Kv3.2 channels. Mol Pharmacol. 2005 May;67(5):1513-21. doi: 10.1124/mol.105.011064. Epub 2005 Feb 11.
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