Anionic glycolipids related to glucuronosyldiacylglycerol inhibit protein kinase Akt

Org Biomol Chem. 2015 Jan 28;13(4):1091-9. doi: 10.1039/c4ob01602e. Epub 2014 Nov 24.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Line, Tumor
  • Glycolipids / chemical synthesis
  • Glycolipids / chemistry*
  • Glycolipids / pharmacology*
  • Humans
  • Inhibitory Concentration 50
  • Protein Kinase Inhibitors / chemical synthesis
  • Protein Kinase Inhibitors / chemistry*
  • Protein Kinase Inhibitors / pharmacology*
  • Protein Structure, Tertiary
  • Proto-Oncogene Proteins c-akt / antagonists & inhibitors*
  • Proto-Oncogene Proteins c-akt / chemistry

Substances

  • Glycolipids
  • Protein Kinase Inhibitors
  • glucuronosyl diacylglycerol
  • Proto-Oncogene Proteins c-akt