title: 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.
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.
authors.affiliation: Department of Medicinal Chemistry, Institute of Pharmacy, Martin-Luther-University Halle-Wittenberg , Halle , Germany and.
authors.forename: Alexander
authors.initials: A
authors.lastname: Rohe
authors.forename: Christiane
authors.initials: C
authors.lastname: Göllner
authors.forename: Frank
authors.initials: F
authors.lastname: Erdmann
authors.forename: Wolfgang
authors.initials: W
authors.lastname: Sippl
authors.forename: Matthias
authors.initials: M
authors.lastname: Schmidt
mesh_terms: D006017:Glycolipids / Q000494:pharmacology*; D006801:Humans; D008565:Membrane Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism*; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors / Q000378:metabolism*; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors / Q000378:metabolism*
chemical_list: C545327:1,2-dipalmitoyl-3-(N-palmitoyl-6-amino-6-deoxyglucosyl)-sn-glycerol; D006017:Glycolipids; D008565:Membrane Proteins; D011505:Protein-Tyrosine Kinases; C490679:PKMYT1 protein, human; D017346:Protein Serine-Threonine Kinases
keywords: Fluorescence polarization; PKMYT1; kinase inhibition