New glucuronosyldiacylglycerol (GlcADG) analogues based on a 2-O-β-D-glucopyranosyl-sn-glycerol scaffold and carrying one or two acyl chains of different lengths have been synthesized as phosphatidylinositol 3-phosphate (PI3P) mimics targeting the protein kinase Akt. Akt inhibitory effect of prepared compounds, was assayed using an in vitro kinase assay. The antiproliferative activity of the compounds was tested in the human ovarian carcinoma IGROV-1 cell line in which we found that two of them could inhibit proliferation, in keeping with the target inhibitory effect.

Anionic glycolipids related to glucuronosyldiacylglycerol inhibit protein kinase Akt / M. Vetro, B. Costa, G. Donvito, N. Arrighetti, L. Cipolla, P. Perego, F. Compostella, F. Ronchetti, D. Colombo. - In: ORGANIC & BIOMOLECULAR CHEMISTRY. - ISSN 1477-0520. - 13:4(2015), pp. 1091-1099. [10.1039/C4OB01602E]

Anionic glycolipids related to glucuronosyldiacylglycerol inhibit protein kinase Akt

M. Vetro
Primo
;
F. Compostella;F. Ronchetti
Penultimo
;
D. Colombo
Ultimo
2015

Abstract

New glucuronosyldiacylglycerol (GlcADG) analogues based on a 2-O-β-D-glucopyranosyl-sn-glycerol scaffold and carrying one or two acyl chains of different lengths have been synthesized as phosphatidylinositol 3-phosphate (PI3P) mimics targeting the protein kinase Akt. Akt inhibitory effect of prepared compounds, was assayed using an in vitro kinase assay. The antiproliferative activity of the compounds was tested in the human ovarian carcinoma IGROV-1 cell line in which we found that two of them could inhibit proliferation, in keeping with the target inhibitory effect.
cancer; domain; acid; 2-O-BETA-D-glucosylglycerol; mechanisms; perifosine; plants
Settore BIO/10 - Biochimica
Settore BIO/14 - Farmacologia
2015
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/243467
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