The glycoglycerolipid 1,2-dipalmitoyl-3-(N-palmitoyl-6'-amino-6'-deoxy-α-d-glucosyl)-sn-glycerol is no inhibitor of the human Myt1 kinase

J Enzyme Inhib Med Chem. 2015 Jun;30(3):514-7. doi: 10.3109/14756366.2014.926343. Epub 2014 Jun 18.

Abstract

Previously, a glycoglycerolipid isolated from marine algae was reported to be a potent and selective inhibitor of the human Myt1 kinase, an enzyme involved in cell cycle regulation with great potential as an anti-cancer target. Based on that report, a lot of research effort has been invested by several working groups to synthesize and derivatize this compound. However, reliable assay data confirming the inhibitory potential and the mechanism of action of these glycoglycerolipids are missing so far. Here, based on experimental data and theoretical considerations, we show that the aforesaid glycoglycerolipid 1,2-dipalmitoyl-3-(N-palmitoyl-6'-amino-6'-deoxy-α-d-glucosyl)-sn-glycerol is not an inhibitor of the human Myt1 kinase.

Keywords: Fluorescence polarization; PKMYT1; kinase inhibition.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Glycolipids / pharmacology*
  • Humans
  • Membrane Proteins / antagonists & inhibitors
  • Membrane Proteins / metabolism*
  • Protein Serine-Threonine Kinases / antagonists & inhibitors
  • Protein Serine-Threonine Kinases / metabolism*
  • Protein-Tyrosine Kinases / antagonists & inhibitors
  • Protein-Tyrosine Kinases / metabolism*

Substances

  • 1,2-dipalmitoyl-3-(N-palmitoyl-6-amino-6-deoxyglucosyl)-sn-glycerol
  • Glycolipids
  • Membrane Proteins
  • Protein-Tyrosine Kinases
  • PKMYT1 protein, human
  • Protein Serine-Threonine Kinases