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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
2008-1-3
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pubmed:abstractText |
Conventional and novel protein kinase C (PKC) isozymes are the main targets of tumor promoters. We developed 1-hexylindolactam-V10 ( 5) as a selective activator for novel PKC isozymes that play important roles in various cellular processes related to tumor promotion, ischemia--reperfusion injury in the heart, and Alzheimer's disease. The compound existed as a mixture of three conformers. The trans-amide restricted analogues of 5 ( 14 and 15) hardly bound to PKC isozymes, suggesting that the active conformation of 5 could be that with a cis-amide. Compound 5 selectively translocated novel PKC isozymes over conventional PKC isozymes in HeLa cells at 0.1-1 microM. These results suggest that 5 could be useful for the functional analysis of novel PKC isozymes.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
10
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pubmed:volume |
51
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
46-56
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pubmed:meshHeading |
pubmed-meshheading:18072722-Cell Membrane,
pubmed-meshheading:18072722-Enzyme Activators,
pubmed-meshheading:18072722-HeLa Cells,
pubmed-meshheading:18072722-Humans,
pubmed-meshheading:18072722-Indoles,
pubmed-meshheading:18072722-Isoenzymes,
pubmed-meshheading:18072722-Lactams,
pubmed-meshheading:18072722-Models, Molecular,
pubmed-meshheading:18072722-Molecular Conformation,
pubmed-meshheading:18072722-Mutation,
pubmed-meshheading:18072722-Protein Binding,
pubmed-meshheading:18072722-Protein Kinase C,
pubmed-meshheading:18072722-Protein Transport,
pubmed-meshheading:18072722-Structure-Activity Relationship
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pubmed:year |
2008
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pubmed:articleTitle |
Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes.
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pubmed:affiliation |
Division of Food Science and Biotechnology, Graduate School of Agriculture, Kyoto University, Kyoto 606-8502, Japan.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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