Document Detail

Structural requirements for the binding of fatty acids to 5-lipoxygenase-activating protein.
MedLine Citation:
PMID:  8088366     Owner:  NLM     Status:  MEDLINE    
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.
S Charleson; J F Evans; S Léger; H Perrier; P Prasit; Z Wang; P J Vickers
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  European journal of pharmacology     Volume:  267     ISSN:  0014-2999     ISO Abbreviation:  Eur. J. Pharmacol.     Publication Date:  1994 May 
Date Detail:
Created Date:  1994-10-19     Completed Date:  1994-10-19     Revised Date:  2004-11-17    
Medline Journal Info:
Nlm Unique ID:  1254354     Medline TA:  Eur J Pharmacol     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  275-80     Citation Subset:  IM    
Department of Biochemistry, Merck Frosst Centre For Therapeutic Research, Pointe Claire-Dorval, Quebec, Canada.
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MeSH Terms
12-Hydroxy-5,8,10,14-eicosatetraenoic Acid
Arachidonic Acid / metabolism*
Binding Sites / drug effects
Carrier Proteins / chemistry,  metabolism*
Hydroxyeicosatetraenoic Acids / pharmacology
Indoles / metabolism
Leukocytes / metabolism*
Leukotrienes / biosynthesis
Membrane Proteins / chemistry,  metabolism*
Quinolines / metabolism
Radioligand Assay
Reg. No./Substance:
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

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