title: Straightforward synthesis of novel Akt inhibitors based on a glucose scaffold.
abstract: Glucose-based analogues of phosphatidylinositol 3-phosphate were straightforwardly synthesised from 2,3,4,6-tetra-O-acetyl-d-glucosyl bromide as protein kinase B (PKB/Akt) inhibitors. beta-d-Glucuronyl diethyl phosphoramidate was identified as a promising hit through biological screening in two different cellular systems. In addition, RNA interference experiments (siRNA) provide evidence of the ability of the compound to exert biological effects specifically through Akt signalling.
authors.affiliation: Department of Biotechnology and Biosciences, University of Milano-Bicocca P.za della Scienza 2, 20126 Milano, Italy. laura.cipolla@unimib.it
authors.forename: Laura
authors.initials: L
authors.lastname: Cipolla
authors.forename: Cristina
authors.initials: C
authors.lastname: Redaelli
authors.forename: Francesca
authors.initials: F
authors.lastname: Granucci
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Zampella
authors.forename: Antonio
authors.initials: A
authors.lastname: Zaza
authors.forename: Riccardo
authors.initials: R
authors.lastname: Chisci
authors.forename: Francesco
authors.initials: F
authors.lastname: Nicotra
mesh_terms: D000818:Animals; D005947:Glucose / Q000737:chemistry*; D007294:Inositol / Q000737:chemistry; D008958:Models, Molecular; D032383:Myocytes, Cardiac / Q000187:drug effects / Q000378:metabolism; D010716:Phosphatidylinositols / Q000737:chemistry; 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 / Q000172:deficiency / Q000235:genetics; D034622:RNA Interference; D051381:Rats
chemical_list: D010716:Phosphatidylinositols; D047428:Protein Kinase Inhibitors; D007294:Inositol; D051057:Proto-Oncogene Proteins c-akt; D005947:Glucose