Synthesis of diacylglycerol analogues as potential second-messenger antagonists and inhibitors of protein kinase C
| Autor: | Alan Lloyd, Ian Gibson, Richard J. K. Taylor, Alan P. Dawson, Silkie Meiners, Jackie Hook, Josie C. Briggs, Alan H. Haines |
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| Rok vydání: | 1992 |
| Předmět: |
Stereochemistry
Second Messenger Systems Biochemistry Analytical Chemistry Diglycerides Tumor Cells Cultured Animals Humans Protein Kinase C Protein kinase C Diacylglycerol kinase chemistry.chemical_classification Molecular Structure biology Organic Chemistry Stereoisomerism Biological activity General Medicine In vitro Rats Enzyme Activation Enzyme chemistry Cell culture Enzyme inhibitor Second messenger system biology.protein Biological Assay |
| Zdroj: | Carbohydrate Research. 234:23-35 |
| ISSN: | 0008-6215 |
| DOI: | 10.1016/0008-6215(92)85036-y |
| Popis: | A series of analogues of diacylglycerol has been prepared and tested as inhibitors of protein kinase C (PKC). The diketone analogues, 10-hydroxymethyl-8,13-eicosanedione (24), 10-acetoxymethyl-8,13-eicosanedione (25), and 10-methoxymethyl-8,13-eicosanedione (26) each inhibited PKC activated by 2-O-acetyl-1-O-oleoylglycerol. Compound 24 was the most effective inhibitor of the growth of MR4 and HT29 cells in culture, and 26 was more effective than 24 against HL60 cells. |
| Databáze: | OpenAIRE |
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