| Structural requirements for the binding of fatty acids to 5-lipoxygenase-activating protein. | |
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MedLine Citation:
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PMID: 8088366 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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5-Lipoxygenase-activating protein is required for cellular leukotriene synthesis and is the target of the leukotriene biosynthesis inhibitors MK-886 (3-[1-(p-chlorophenyl)-5-isopropyl-3-tert-butylthio-1H- indol-2-yl]-2,2-dimethylpropanoic acid) and MK-591 (3-[1-(4-chlorobenzyl)-3-(t-butylthio)-5-(quinolin-2-ylmethoxy)-indol-2-yl] - 2,2-dimethylpropanoic acid). Recent studies demonstrate that 5-lipoxygenase-activating protein binds arachidonic acid and stimulates the utilization of this substrate by 5-lipoxygenase. The present study utilizes a radioligand binding assay to assess the affinity of 5-lipoxygenase-activating protein for arachidonic acid and the specificity of the fatty acid binding site on 5-lipoxygenase-activating protein. Our findings demonstrate that the presence of a free carboxyl group on fatty acids or leukotriene biosynthesis inhibitors which interact with 5-lipoxygenase-activating protein is not required for specific binding to the protein. However, the degree of saturation significantly affects the affinity of fatty acids for 5-lipoxygenase-activating protein. |
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Authors:
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S Charleson; J F Evans; S Léger; H Perrier; P Prasit; Z Wang; P J Vickers |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: European journal of pharmacology Volume: 267 ISSN: 0014-2999 ISO Abbreviation: Eur. J. Pharmacol. Publication Date: 1994 May |
Date Detail:
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Created Date: 1994-10-19 Completed Date: 1994-10-19 Revised Date: 2004-11-17 |
Medline Journal Info:
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Nlm Unique ID: 1254354 Medline TA: Eur J Pharmacol Country: NETHERLANDS |
Other Details:
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Languages: eng Pagination: 275-80 Citation Subset: IM |
Affiliation:
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Department of Biochemistry, Merck Frosst Centre For Therapeutic Research, Pointe Claire-Dorval, Quebec, Canada. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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12-Hydroxy-5,8,10,14-eicosatetraenoic Acid Arachidonic Acid / metabolism* Binding Sites / drug effects Carrier Proteins / chemistry, metabolism* Humans Hydroxyeicosatetraenoic Acids / pharmacology Indoles / metabolism Leukocytes / metabolism* Leukotrienes / biosynthesis Membrane Proteins / chemistry, metabolism* Quinolines / metabolism Radioligand Assay |
| Chemical | |
Reg. No./Substance:
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0/5-lipoxygenase-activating protein; 0/Carrier Proteins; 0/Hydroxyeicosatetraenoic Acids; 0/Indoles; 0/Leukotrienes; 0/Membrane Proteins; 0/Quinolines; 118414-82-7/L 663536; 136668-42-3/MK 0591; 136668-70-7/L 691831; 506-32-1/Arachidonic Acid; 59985-28-3/12-Hydroxy-5,8,10,14-eicosatetraenoic Acid; 73945-47-8/15-hydroxy-5,8,11,13-eicosatetraenoic acid |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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