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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
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pubmed:dateCreated |
1992-7-14
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pubmed:abstractText |
The rat liver microsomal vitamin K-dependent carboxylase catalyzes the carboxylation of glutamyl to gamma-carboxyglutamyl residues in the presence of reduced vitamin K, O2 and CO2. The specificity of the enzyme for the vitamin substrate has been probed by the synthesis of a series of fluoro- hydroxy- and methoxy-analogs. 2-Fluoro-methyl-3-phytyl-1,4-naphthoquinone and 2-methyl-3-(1'-fluorodecyl)-1,4-naphthoquinone were synthesized but found to be unstable under enzyme assay conditions. The reduced (naphthohydroquinone) forms of 2-hydroxy-methyl-3-phytyl-1,4-naphthoquinone, 2-methoxymethyl-3-phytyl-1,4-naphthoquinone and 2-methyl-3-(1'-hydroxy-decyl)-1,4-naphthoquinone were inactive as substrates, but inhibitors of the enzyme. The two hydroxy analogs were shown to be low Ki (less than 10 microM) inhibitors of the reduced 2-methyl-3-phytyl-1,4-naphthoquinone-dependent activity of the enzyme. The oxidized forms of these compounds did not inhibit the enzyme and they had no activity as in vivo anticoagulants.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
0951-6433
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
3
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
205-9
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:1599614-Animals,
pubmed-meshheading:1599614-Carbon-Carbon Ligases,
pubmed-meshheading:1599614-Ligases,
pubmed-meshheading:1599614-Male,
pubmed-meshheading:1599614-Microsomes, Liver,
pubmed-meshheading:1599614-Rats,
pubmed-meshheading:1599614-Rats, Inbred Strains,
pubmed-meshheading:1599614-Vitamin K
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pubmed:year |
1992
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pubmed:articleTitle |
Synthesis of fluoro- and hydroxy-derivatives of vitamin K as substrates or inhibitors of the liver microsomal vitamin K-dependent carboxylase.
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pubmed:affiliation |
Department of Biochemistry, College of Agricultural and Life Sciences, University of Wisconsin-Madison 53706.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, U.S. Gov't, Non-P.H.S.,
Research Support, Non-U.S. Gov't
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