Apamin

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Apamin ( Apis mellifera )
Mass / length primary structure 18 amino acids
Identifier
Gene name (s) GB18161
External IDs
Occurrence
Parent taxon Bees, scorpions

Apamin refers to a neurotoxic peptide contained in bee venom , which consists of 18 amino acid residues .

It binds in a specific way to calcium-dependent potassium channels , the so-called SK channels ( small conductance ), which can not be inhibited by tetraethylammonium , and thereby blocks them. These channels are responsible for post-hyperpolarization after the action potential . Apamin is used as a marker for this type of channel in experimental neuroscience.

literature

  • E. Habermann: Apamin. In: Pharmacol. Ther. 25 (2), 1984, pp. 255-270. doi: 10.1016 / 0163-7258 (84) 90046-9 . PMID 6095335 .
  • DJ Son, JW Lee, YH Lee, HS Song, CK Lee, JT Hong: Therapeutic application of anti-arthritis, pain-releasing, and anti-cancer effects of bee venom and its constituent compounds. In: Pharmacol. Ther. 115 (2), August 2007, pp. 246-270. doi: 10.1016 / j.pharmthera.2007.04.004 . PMID 17555825 .
  • NA Castle, DG Haylett, DH Jenkinson: Toxins in the characterization of potassium channels. In: Trends Neurosci. 12 (2), February 1989, pp. 59-65. doi: 10.1016 / 0166-2236 (89) 90137-9 . PMID 2469212 .
  • AJ Kastin: Apamin. In: handbook of biologically active peptides. 2013, pp. 417-418.
  • J. Vincent, H. Schweitz, M. Lazdunski: Structure-Function Relationships and Site of Action of Apamin, a Neurotoxic Polypeptide of Bee Venom with an Action on the Central Nervous System. In: Biochemistry. 14 (11), 1975, pp. 2521-2525. doi: 10.1021 / bi00682a035 .
  • M. Stocker, M. Krause, P. Pedarzani: An apamin-sentisitive Ca2 + -activated K + current in hippocampal pyramidal neurons. In: PNAS. 96 (8), 1999.
  • M. Stocker: Ca (2 +) - activated K + channels: molecular determinants and function of the SK family. In: Nat. Rev. Neurosci. 5 (10), October 2004, pp. 758-770. doi: 10.1038 / nrn1516 . PMID 15378036 .
  • A. Nolting, T. Ferraro, D. D'hoedt, M. Stocker: An Amino Acid Outside the Pore Region Influences Apamin Sensitivity in Small Conductance Ca2 + -activated K + Channels. In: J. Biol. Chem. 282 (6), February 2007, pp. 3478-3486. doi: 10.1074 / jbc.M607213200 . PMC 1849974 (free full text). PMID 17142458 .
  • D. Cheng-Raude, M. Treloar, E. Habermann: Preparation and pharmacokinetics of labeled derivatives of apamin. In: Toxicon. 14 (6), 1976, pp. 467-476. doi: 10.1016 / 0041-0101 (76) 90064-7 .
  • R. Saravanan, R. King, J. White: Transient claw hand owing to a bee sting. A report of two cases. In: J Bone Joint Surg Br. 86 (3), April 2004, pp. 404-405. doi: 10.1302 / 0301-620x.86b3.14311 . PMID 15125129 .
  • E. Habermann: Neurotoxicity of Apamin and MCD Peptide upon Central Application. In: archives of pharmacology. (300), 1977, pp. 189-191.
  • G. Lallement, P. Fosbraey, V. Baille-Le-Crom, JE Tattersall, G. Blanchet, JR Wetherell, P. Rice, SL Passingham, H. Sentenac-Roumanou: Compared toxicity of the potassium channel blockers, apamin and dendrotoxin . In: Toxicology. 104 (1-3), December 1995, pp. 47-52. doi: 10.1016 / 0300-483X (95) 03120-5 . PMID 8560501 .
  • ESL Faber, P. Sah: Functions of SK channels in central neurons. In: Clinical and experimental pharmacology and physiology. 34 (10), V, pp. 1077-1083. doi: 10.1111 / j.1440-1681.2007.04725.x . PMID 17714097 .
  • M. Moreno, E. Giralt: Three valuable peptides from bee and wasp venoms for therapeutic and biotechnological use: melittin, apamin and mastoparan. In: Toxins. Volume 7, number 4, April 2015, pp. 1126-1150, doi : 10.3390 / toxins7041126 , PMID 25835385 , PMC 4417959 (free full text) (review).