| Inhibition of Drosophila acetylcholinesterase by 7-(methylethoxyphosphinyloxy)1-methyl-quinolinium iodide. | |
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MedLine Citation:
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PMID: 10421448 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The kinetic behaviour of Drosophila melanogaster acetylcholinesterase toward its substrate shows, in comparison with classic Michaelis-Menten kinetics, an apparent homotropic cooperative double activation-inhibition pattern. In order to construct an appropriate kinetic model and obtain further information on the mechanism of the catalytic action of this enzyme, the hydrolysis of acetylthiocholine in the absence and presence of different concentrations of synthetic quaternary methylphosphonate, 7-(methylethoxyphosphinyloxy)1-methyl-quinolinium iodide (MEPQ), was followed on a stopped-flow apparatus. The reaction at low substrate concentrations was followed until the change of the absorbance became negligible and at high concentrations only initial parts were recorded. A simultaneous analysis of the progress curves using numerical integration showed that the powerful organophosphonate inhibitor binds and compete with the substrate for the same binding sites. The results are also in accordance with the hypothesis that virtually every substrate or quasi-substrate molecule that enters into the gorge of active site is hydrolysed. |
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Authors:
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J Stojan; V Marcel; D Fournier |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Chemico-biological interactions Volume: 119-120 ISSN: 0009-2797 ISO Abbreviation: Chem. Biol. Interact. Publication Date: 1999 May |
Date Detail:
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Created Date: 1999-08-19 Completed Date: 1999-08-19 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 0227276 Medline TA: Chem Biol Interact Country: IRELAND |
Other Details:
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Languages: eng Pagination: 147-57 Citation Subset: IM |
Affiliation:
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Institute of Biochemistry, Medical Faculty, University of Ljubljana, Slovenia. stojan@ibmi.mf.uni-lj.si |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Acetylcholinesterase
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metabolism Acetylthiocholine / metabolism Animals Brain / enzymology Catalysis Cholinesterase Inhibitors / pharmacokinetics, pharmacology* Drosophila melanogaster / enzymology* Hydrolysis Kinetics Models, Chemical Models, Molecular Phosphorylation Quinolinium Compounds / pharmacokinetics, pharmacology* |
| Chemical | |
Reg. No./Substance:
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0/Cholinesterase Inhibitors; 0/Quinolinium Compounds; 4468-05-7/Acetylthiocholine; 95230-44-7/7-((methylethoxyphosphinyl)oxy)-1-methylquinolinium; EC 3.1.1.7/Acetylcholinesterase |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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