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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
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pubmed:dateCreated |
1998-6-19
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pubmed:abstractText |
It has been shown that melatonin through binding to calmodulin acts both in vitro and in vivo as a potent calmodulin antagonist. It is known that calmodulin antagonists both bind to the hydrophobic domain of Ca2+ activated calmodulin, and inhibit protein kinase C activity. In this work we explored the effects of melatonin on Ca2+ dependent protein kinase C activity in vitro using both a pure commercial rat brain protein kinase C, and a partially purified enzyme from MDCK and N1E-115 cell homogenates. The results showed that melatonin directly activated protein kinase C with a half stimulatory concentration of 1 nM. In addition the hormone augmented by 30% the phorbol ester stimulated protein kinase C activity and increased [3H] PDBu binding to the kinase. In contrast, calmodulin antagonists (500 microM) and protein kinase C inhibitors (100 microM) abolished the enzyme activity. Melatonin analogs tested were ineffective in increasing either protein kinase C activity or [3H] PDBu binding. Moreover, the hormone stimulated protein kinase C autophosphorylation directly and in the presence of phorbol ester and phosphatidylserine. The results show that besides the melatonin binding to calmodulin, the hormone also interacts with protein kinase C only in the presence of Ca2+. They also suggest that the melatonin mechanism of action may involve interactions with other intracellular hydrophobic and Ca2+ dependent proteins.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Calmodulin,
http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Melatonin,
http://linkedlifedata.com/resource/pubmed/chemical/Phorbol 12,13-Dibutyrate,
http://linkedlifedata.com/resource/pubmed/chemical/Protein Kinase C
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pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
0364-3190
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
23
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
601-6
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pubmed:dateRevised |
2007-11-15
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pubmed:meshHeading |
pubmed-meshheading:9566597-Animals,
pubmed-meshheading:9566597-Brain,
pubmed-meshheading:9566597-Calmodulin,
pubmed-meshheading:9566597-Cell Line,
pubmed-meshheading:9566597-Enzyme Activation,
pubmed-meshheading:9566597-Enzyme Inhibitors,
pubmed-meshheading:9566597-Kinetics,
pubmed-meshheading:9566597-Melatonin,
pubmed-meshheading:9566597-Phorbol 12,13-Dibutyrate,
pubmed-meshheading:9566597-Protein Binding,
pubmed-meshheading:9566597-Protein Kinase C,
pubmed-meshheading:9566597-Rats
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pubmed:year |
1998
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pubmed:articleTitle |
In vitro stimulation of protein kinase C by melatonin.
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pubmed:affiliation |
Universidad Autónoma Metropolitana-Iztapalapa, Departamento de Biología de la Reproducción, CBS, Mexico DF, Mexico. fat@xanum.uam.mx
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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