A Novel Water-Soluble Phosphonate Analog of Phosphatidylinositol, D-Myo-Inositol4-(Hexadecyloxy)-3(5)-Methoxybutanephosphonate (C4-PI), Inhibits Epithelial Cell Proliferation and is a Substrate but not an Inhibitor of Phosphatidylinositol 3-Kinase

Autor:	Robert Bittman, Lawrence W. Leung, Christina Richard, Gilbert Arthur, Weiyang Lin
Rok vydání:	1998
Předmět:	Phospholipase C Kinase Pharmaceutical Science Biology Molecular biology Phosphonate Isozyme In vitro chemistry.chemical_compound Biochemistry chemistry Pi Phosphorylation Phosphatidylinositol
Zdroj:	Journal of Liposome Research. 8:213-224
ISSN:	1532-2394 0898-2104
DOI:	10.3109/08982109809035527
Popis:	D-myo-Inositol 4-(hexadecyloxy)-3(S)-methoxybutanephosphonate (C4-PI), a water soluble isosteric phosphonate analog of phosphatidylinositol (PI) that is not a substrate of phosphatidylinositol-specific phospholipase C isozymes, was synthesized and was found to be phosphorylated by phosphatidyl-inositol 3-kinase (PI 3-kinase) activity immunoprecipitated from insulin-stimulated cells. The extent of phosphorylation of C4-PI was similar to or greater than that of phosphatidylinositol, especially at higher concentrations. Since C4-PI is very water soluble, it is an attractive tool for assaying PI kinases in vitro as no detergent or sonication is required in contrast to assays with the long-chain PI which forms micelles. The extent of phosphorylation of C4-PI was similar or greater than that of PI, especially at higher concentrations. C4-PI was, at best, a poor inhibitor of of PI 3-kinase activity (IC50 > 150 µM). C4-PI exhibited antiproliferative properties against the neuroblastoma cell lines SK-N-SH ...
Databáze:	OpenAIRE
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