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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
9
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pubmed:dateCreated |
1984-10-3
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pubmed:abstractText |
A series of peptides that contain an N-terminal 2-methyl-1,4-naphthoquinone group or analogues of this structure have been prepared as potential substrates or inhibitors of the rat liver microsomal vitamin K dependent carboxylase. The parent compound, gamma-2-(methyl-1,4-naphthoquinonyl-3)butyryl-Glu-Glu-Leu-OMe, is a good substrate for the carboxylase at low concentrations and has a Km of about 50 microM. This is roughly 2 orders of magnitude lower than the Km of most simple peptide substrates that have been synthesized. Replacement of the 2-methyl-1,4-naphthoquinone group with its desmethyl analogue, a naphthyl, or a stearyl group decreased substrate effectiveness. At higher concentrations, the parent compound and its desmethyl analogue were potent inhibitors of the vitamin K dependent carboxylation reaction. The degree of inhibition exhibited by these peptides was dependent on the vitamin KH2 concentration of the incubation.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/1-Carboxyglutamic Acid,
http://linkedlifedata.com/resource/pubmed/chemical/Calcium-Binding Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Carbon-Carbon Ligases,
http://linkedlifedata.com/resource/pubmed/chemical/Ligases,
http://linkedlifedata.com/resource/pubmed/chemical/Naphthoquinones,
http://linkedlifedata.com/resource/pubmed/chemical/Oligopeptides,
http://linkedlifedata.com/resource/pubmed/chemical/Osteocalcin,
http://linkedlifedata.com/resource/pubmed/chemical/glutamyl carboxylase
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
27
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1196-201
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:6332196-1-Carboxyglutamic Acid,
pubmed-meshheading:6332196-Calcium-Binding Proteins,
pubmed-meshheading:6332196-Carbon-Carbon Ligases,
pubmed-meshheading:6332196-Kinetics,
pubmed-meshheading:6332196-Ligases,
pubmed-meshheading:6332196-Naphthoquinones,
pubmed-meshheading:6332196-Oligopeptides,
pubmed-meshheading:6332196-Osteocalcin,
pubmed-meshheading:6332196-Structure-Activity Relationship
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pubmed:year |
1984
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pubmed:articleTitle |
Derivatives of 2-methyl-1,4-naphthoquinone as substrates and inhibitors of the vitamin K dependent carboxylase.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
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