Modulation of the cytosolic Ca++ concentration by alkylphospho-L-serine analogs: relation to their antiproliferative action
| Autor: | Christine Vollgraf, Jutta Bergmanna, Ilse Junghahn, P. Langen, Hans Brachwitz |
|---|---|
| Rok vydání: | 1997 |
| Předmět: |
Alkylation
Stereochemistry Immunology Stimulation L serine Phosphatidylserines Inhibitory postsynaptic potential Epithelium Serine Structure-Activity Relationship Cytosol medicine Potency Humans Breast Alkyl Cell Line Transformed Pharmacology chemistry.chemical_classification Dose-Response Relationship Drug Molecular Structure Chemistry medicine.anatomical_structure Cytosolic ca Calcium Cell Division |
| Zdroj: | Journal of lipid mediators and cell signalling. 15(2) |
| ISSN: | 0929-7855 |
| Popis: | Antiproliferative alkyllysophospholipid (ALP) analogs produced multiple effects on the cytosolic Ca + + concentration ([Ca + + ] i ) in an immortalized human breast epithelial cell line (H 184). The addition of small concentrations resulted in a short transient [Ca + + ] i response. With higher concentrations the transient rise was followed by a sustained increase. Pretreatment of cells with the ALP analogs for two minutes inhibited the transient [Ca + + ] response. Increases in [Ca + + ] i and inhibition of the transient increase were studied in relation to the dose and structure of several ALP analogs. In a series of alkylphospho- l -serine analogs with different lengths of the alkyl chain we found different dependencies of the stimulatory and inhibitory effects on the dose and the structure. The ability to increase [Ca ++ ] i is absent with the C 14 and C 15 analogs, is low with the C 16 and high with the C 18 analog. With the exception of the C 12 analog, a dose-related inhibition was observed with all derivatives but the effective concentrations differed very strongly and the maximal potency was reached with the C 15 and C 16 analogs. The antiproliferative action seems to correlate rather with the potency to inhibit the transient [Ca + + ]; response than with its stimulation. |
| Databáze: | OpenAIRE |
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