A metabolite of an antineoplastic ether phospholipid may inhibit transmembrane signalling via protein kinase C View Full Text


Ontology type: schema:ScholarlyArticle     


Article Info

DATE

1987-11

AUTHORS

Wim J. van Blitterswijk, Rob L. van der Bend, Ïjsbrand M. Kramer, Arthur J. Verhoeven, Henk Hilkmann, John de Widt

ABSTRACT

In our search for the mechanisms by which the drug 1-O-alkyl-2-O-methylglycero-3-phosphocholine (AMG-PC) inhibits tumor growth and metastasis, we have detected a metabolite, 1-O-alkyl-2-O-methylglycerol (AMG), in membranes of MO4 mouse fibrosarcoma cells grown in the presence of the drug. Synthetic AMG inhibited the activation of highly purified human protein kinase C by diacylglycerol in the presence of phosphatidylserine. Furthermore, AMG also inhibited the receptor-specific binding of 3H-phorbol-12,13-dibutyrate to human HL-60 promyeloid leukemia cells in a dose-dependent fashion. AMG-PC was not effective or much less so in these assays. We suggest that interaction of the metabolite AMG with protein kinase C may inhibit stimulus-response coupling in tumor cells and may thus potentially contribute to the mechanism by which AMG-PC exerts its anticancer activities. More... »

PAGES

842-846

Identifiers

URI

http://scigraph.springernature.com/pub.10.1007/bf02535541

DOI

http://dx.doi.org/10.1007/bf02535541

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1011440683

PUBMED

https://www.ncbi.nlm.nih.gov/pubmed/3444375


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