title: Kinetics of the ceramide kinase inhibitor K1, a suppressor of mast-cell activation.
abstract: In a previous study, we synthesized a novel inhibitor of ceramide kinase, K1. In this study, we determined that inhibition by K1 is non-competitive and that four intact six-membered rings are important to the inhibitory activity. Furthermore, we identified an effective in vivo concentration for K1, at which it did not influence any cellular lipid synthesis other than that of ceramide 1-phosphate (C1P) using RBL-2H3 cells, and found that K1 suppressed the activation of mast cells.
authors.affiliation: Laboratory of Biomembrane and Biofunctional Chemistry, Faculty of Pharmaceutical Science and Faculty of Advanced Life Sciences, Hokkaido University, Japan.
authors.forename: Hirotaka
authors.initials: H
authors.lastname: Kumada
authors.forename: Susumu
authors.initials: S
authors.lastname: Mitsutake
authors.forename: Yuichi
authors.initials: Y
authors.lastname: Inagaki
authors.forename: Shino
authors.initials: S
authors.lastname: Mitsunaga
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Tsuchikawa
authors.forename: Shigeo
authors.initials: S
authors.lastname: Katsumura
authors.forename: Yasuyuki
authors.initials: Y
authors.lastname: Igarashi
mesh_terms: D000818:Animals; D000001:Calcimycin / Q000494:pharmacology; D002250:Carbon Radioisotopes / Q000378:metabolism; D045744:Cell Line, Tumor; D002855:Chromatography, Thin Layer; D004305:Dose-Response Relationship, Drug; D007476:Ionophores / Q000494:pharmacology; D007700:Kinetics; D015471:Leukemia, Basophilic, Acute / Q000201:enzymology; D008407:Mast Cells / Q000187:drug effects* / Q000378:metabolism; D015394:Molecular Structure; D017853:Phosphotransferases (Alcohol Group Acceptor) / Q000037:antagonists & inhibitors*; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats
chemical_list: D002250:Carbon Radioisotopes; D007476:Ionophores; D047428:Protein Kinase Inhibitors; D000001:Calcimycin; D017853:Phosphotransferases (Alcohol Group Acceptor); C066324:ceramide kinase