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. VetroPrimo
;F. Compostella;F. RonchettiPenultimo
;D. ColomboUltimo
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.File | Dimensione | Formato | |
---|---|---|---|
c4ob01602e.pdf
accesso aperto
Descrizione: ArticleRonchetti
Tipologia:
Post-print, accepted manuscript ecc. (versione accettata dall'editore)
Dimensione
822.42 kB
Formato
Adobe PDF
|
822.42 kB | Adobe PDF | Visualizza/Apri |
Org. Biomol. Chem., 2015, 13, 1091.pdf
accesso aperto
Descrizione: articolo
Tipologia:
Publisher's version/PDF
Dimensione
519.45 kB
Formato
Adobe PDF
|
519.45 kB | Adobe PDF | Visualizza/Apri |
Pubblicazioni consigliate
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.