Literature DB >> 7925953

Two-step binding of green mamba toxin to muscarinic acetylcholine receptor.

T Toomela1, M Jolkkonen, A Rinken, J Järv, E Karlsson.   

Abstract

The mechanism of binding of toxin MT2 from venom of green mamba Dendroaspis angusticeps to muscarinic acetylcholine receptors from rat cerebral cortex was investigated by studying the kinetics of the toxin-receptor interaction. The muscarinic antagonist N-methyl-[3H]scopolamine was used as a 'reporter' ligand. Evidence for a mechanism of toxin-receptor interaction comprising at least two steps was obtained. Such a mechanism increases the potency of the toxin. The first step was fast with no competition between the toxin and the antagonist. The second step was slow with formation of a more stable toxin-receptor complex and inhibition of the antagonist binding. It is proposed that the snake toxin is a muscarinic agonist of slow action.

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Year:  1994        PMID: 7925953     DOI: 10.1016/0014-5793(94)00926-0

Source DB:  PubMed          Journal:  FEBS Lett        ISSN: 0014-5793            Impact factor:   4.124


  4 in total

Review 1.  On the different experimental manifestations of two-state 'induced-fit' binding of drugs to their cellular targets.

Authors:  Georges Vauquelin; Isabelle Van Liefde; David C Swinney
Journal:  Br J Pharmacol       Date:  2016-03-15       Impact factor: 8.739

2.  Adrenoceptor activity of muscarinic toxins identified from mamba venoms.

Authors:  K Näreoja; J P Kukkonen; S Rondinelli; D M Toivola; J Meriluoto; J Näsman
Journal:  Br J Pharmacol       Date:  2011-09       Impact factor: 8.739

3.  SLEEPLESS is a bifunctional regulator of excitability and cholinergic synaptic transmission.

Authors:  Meilin Wu; James E Robinson; William J Joiner
Journal:  Curr Biol       Date:  2014-03-06       Impact factor: 10.834

4.  Three-fingered RAVERs: Rapid Accumulation of Variations in Exposed Residues of snake venom toxins.

Authors:  Kartik Sunagar; Timothy N W Jackson; Eivind A B Undheim; Syed A Ali; Agostinho Antunes; Bryan G Fry
Journal:  Toxins (Basel)       Date:  2013-11-18       Impact factor: 4.546

  4 in total

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