Peptide Information

General Information of This Peptide
Peptide ID
BTDP008609
Peptide Name
Apamin
Symonym
Apamine
Species
Apis mellifera (Honeybee)
Uniprot Name
APAM_APIME
Alphafold ID
P01500
3D Structure
Download
2D Sequence
3D Structure
Source
RSCB PDB: 7OXF
Sequence
MISMLRCIYLFLSVILITSYFVTPVMPCNCKAPETALCARRCQQHG
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Sequence Length
46
Mass (Da)
5223
Signal Sequence
MISMLRCIYLFLSVILITSYFVTPVMP
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Sequence Removed Signal Peptide
CNCKAPETALCARRCQQHG
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Disulfide Bond
28-38;30-42
PDB ID
7OXF
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Kingdom: Metazoa
Phylum: Arthropoda
Class: Insecta
Order: Hymenoptera
Family: Apidae
Genus: Apis
Species: Apis mellifera
Full List of Activity Data of This Peptide Toxin
                        Target Name Activity Data Type Activity Data Concentration Note Reference
 Target Info    KCa2 Dissociation constant
4 pM
 . . [1- 18]
 Target Info    KCa2.3 Dissociation constant
0.011 nM
 . . [1- 18]
 Target Info    KCa2 Dissociation constant
0.012 nM
 . . [1- 18]
 Target Info    KCa2.1 Dissociation constant
0.39 nM
 . . [1- 18]
 Target Info    Kir2.1 Dissociation constant
20 μM
 . . [1- 18]
 Target Info    Kv1.2 Inhibition rate .
5 μM
 . [1- 18]
 Target Info    Kv7.1 Inhibition rate .
5 μM
 . [1- 18]
 Target Info    Shaker-IR Inhibition rate .
5 μM
 . [1- 18]
 Target Info    KCa3.1 Inhibition rate .
5 μM
 . [1- 18]
 Target Info    Kv1.4 Inhibition rate .
5 μM
 . [1- 18]
 Target Info    Kv1 Inhibition rate .
5 μM
 . [1- 18]
 Target Info    Kv1.6 Inhibition rate .
5 μM
 . [1- 18]
 Target Info    Kv1.5 Inhibition rate .
5 μM
 . [1- 18]
 Target Info    Kv1.3 Inhibition rate .
5 μM
 . [1- 18]
 Target Info    Kv3.1 Inhibition rate .
5 μM
 . [1- 18]
 Target Info    Kv7.1 Inhibition rate .
5 μM
 . [1- 18]
 Target Info    Kv4.3 Inhibition rate .
5 μM
 . [1- 18]
 Target Info    Kv11 Inhibition rate .
5 μM
 . [1- 18]
 Target Info    Kv10 Inhibition rate .
5 μM
 . [1- 18]
 Target Info    KCa1.1 Inhibition rate .
5 μM
 . [1- 18]
 Target Info    Kv2.1 Inhibition rate .
5 μM
 . [1- 18]
 Target Info    Kv7.2/7.3 Inhibition rate .
5 μM
 . [1- 18]
 Target Info    Kir3.1/3.2 Inhibition rate .
5 μM
 . [1- 18]
 Target Info    Kir3.1/3.4 Inhibition rate
20 %
1 μM
 . [1- 18]
 Target Info    KCa2.2 IC50
27 - 140 pM
 . . [1- 20]
 Target Info    KCa2 IC50
0.024 nM
 . . [1- 18]
 Target Info    KCa2 IC50
0.088 nM
 . . [1- 18]
 Target Info    KCa2.3 IC50
0.6 - 4 nM
 . . [1- 20]
 Target Info    KCa2.3 IC50
0.6 - 4 nM
 . . [1- 20]
 Target Info    KCa2.1 IC50
0.7 - 12 nM
 . . [1- 20]
 Target Info    KCa2.3 IC50
2.3 nM
 . . [1- 18]
 Target Info    KCa2.3 IC50
4 nM
 . . [1- 18]
 Target Info    KCa2.1 IC50
4.1 nM
 . . [1- 18]
 Target Info    Kv1.3 IC50
13 nM
 . . [1- 20]
 Target Info    KCa2.2 IC50
27 - 140 nM
 . . [1- 20]
 Target Info    KCa2 IC50
27 - 140 nM
 . . [1- 20]
 Target Info    KCa2.1 IC50
28 nM
 . . [1- 20]
 Target Info    KCa2.1 IC50
196 nM
 . . [1- 18]
References
Ref 1 The precursors of the bee venom constituents apamin and MCD peptide are encoded by two genes in tandem which share the same 3'-exon. J Biol Chem. 1995 May 26;270(21):12704-8. doi: 10.1074/jbc.270.21.12704.
Ref 2 The peptide components of bee venom. Eur J Biochem. 1976 Jan 15;61(2):369-76. doi: 10.1111/j.1432-1033.1976.tb10030.x.
Ref 3 Apamin as a selective blocker of the calcium-dependent potassium channel in neuroblastoma cells: voltage-clamp and biochemical characterization of the toxin receptor. Proc Natl Acad Sci U S A. 1982 Feb;79(4):1308-12. doi: 10.1073/pnas.79.4.1308.
Ref 4 Apamin, a blocker of the calcium-activated potassium channel, induces neurodegeneration of Purkinje cells exclusively. Brain Res. 1997 Dec 19;778(2):405-8. doi: 10.1016/s0006-8993(97)01165-7.
Ref 5 Determinants of apamin and d-tubocurarine block in SK potassium channels. J Biol Chem. 1997 Sep 12;272(37):23195-200. doi: 10.1074/jbc.272.37.23195.
Ref 6 Pharmacological characterization of small-conductance Ca(2+)-activated K(+) channels stably expressed in HEK 293 cells. Br J Pharmacol. 2000 Mar;129(5):991-9. doi: 10.1038/sj.bjp.0703120.
Ref 7 SK3 is an important component of K(+) channels mediating the afterhyperpolarization in cultured rat SCG neurones. J Physiol. 2001 Sep 1;535(Pt 2):323-34. doi: 10.1111/j.1469-7793.2001.00323.x.
Ref 8 Apamin interacts with all subtypes of cloned small-conductance Ca2+-activated K+ channels. Pflugers Arch. 2001 Jan;441(4):544-50. doi: 10.1007/s004240000447.
Ref 9 An amino acid outside the pore region influences apamin sensitivity in small conductance Ca2+-activated K+ channels. J Biol Chem. 2007 Feb 9;282(6):3478-86. doi: 10.1074/jbc.M607213200. Epub 2006 Dec 1.
Ref 10 Apamin reduces neuromuscular transmission by activating inhibitory muscarinic M(2) receptors on motor nerve terminals. Eur J Pharmacol. 2010 Jan 25;626(2-3):239-43. doi: 10.1016/j.ejphar.2009.09.064. Epub 2009 Oct 8.
Ref 11 Allosteric block of KCa2 channels by apamin. J Biol Chem. 2010 Aug 27;285(35):27067-27077. doi: 10.1074/jbc.M110.110072. Epub 2010 Jun 18.
Ref 12 The small neurotoxin apamin blocks not only small conductance Ca(2+) activated K(+) channels (SK type) but also the voltage dependent Kv1.3 channel. Eur Biophys J. 2017 Sep;46(6):517-523. doi: 10.1007/s00249-016-1196-0. Epub 2017 Jan 20.
Ref 13 Apamin inhibits TNF-- and IFN--induced inflammatory cytokines and chemokines via suppressions of NF-B signaling pathway and STAT in human keratinocytes. Pharmacol Rep. 2017 Oct;69(5):1030-1035. doi: 10.1016/j.pharep.2017.04.006. Epub 2017 Apr 18.
Ref 14 Apamin Suppresses LPS-Induced Neuroinflammatory Responses by Regulating SK Channels and TLR4-Mediated Signaling Pathways. Int J Mol Sci. 2020 Jun 17;21(12):4319. doi: 10.3390/ijms21124319.
Ref 15 Apamin from bee venom suppresses inflammation in a murine model of gouty arthritis. J Ethnopharmacol. 2020 Jul 15;257:112860. doi: 10.1016/j.jep.2020.112860. Epub 2020 Apr 11.
Ref 16 Antioxidative, Antiapoptotic, and Anti-Inflammatory Effects of Apamin in a Murine Model of Lipopolysaccharide-Induced Acute Kidney Injury. Molecules. 2020 Dec 3;25(23):5717. doi: 10.3390/molecules25235717.
Ref 17 Solution structure of apamin determined by nuclear magnetic resonance and distance geometry. Biochemistry. 1988 Nov 1;27(22):8491-8. doi: 10.1021/bi00422a029.
Ref 18 Binding and toxicity of apamin. Characterization of the active site. Eur J Biochem. 1991 Mar 28;196(3):639-45. doi: 10.1111/j.1432-1033.1991.tb15860.x.
Ref 19 [Sequence analysis of bee venom neurotoxin (apamine) from its tryptic and chymotryptic cleavage products]. Hoppe Seylers Z Physiol Chem. 1967 Jun;348(6):737-8.
Ref 20 [Spatial structure of apamin in solution]. Mol Biol (Mosk). 1991 Jul-Aug;25(4):937-45.
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