title: Anionic glycolipids related to glucuronosyldiacylglycerol inhibit protein kinase Akt.
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. The Akt inhibitory effect of the 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.
authors.affiliation: Dipartimento di Biotecnologie Mediche e Medicina Traslazionale, Università degli Studi di Milano, Via Saldini 50, 20133 Milano, Italy. diego.colombo@unimi.it.
authors.forename: Maria
authors.initials: M
authors.lastname: Vetro
authors.forename: Barbara
authors.initials: B
authors.lastname: Costa
authors.forename: Giulia
authors.initials: G
authors.lastname: Donvito
authors.forename: Noemi
authors.initials: N
authors.lastname: Arrighetti
authors.forename: Laura
authors.initials: L
authors.lastname: Cipolla
authors.forename: Paola
authors.initials: P
authors.lastname: Perego
authors.forename: Federica
authors.initials: F
authors.lastname: Compostella
authors.forename: Fiamma
authors.initials: F
authors.lastname: Ronchetti
authors.forename: Diego
authors.initials: D
authors.lastname: Colombo
mesh_terms: D045744:Cell Line, Tumor; D006017:Glycolipids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D017434:Protein Structure, Tertiary; D051057:Proto-Oncogene Proteins c-akt / Q000037:antagonists & inhibitors* / Q000737:chemistry
chemical_list: D006017:Glycolipids; D047428:Protein Kinase Inhibitors; C014573:glucuronosyl diacylglycerol; D051057:Proto-Oncogene Proteins c-akt