Kinetics of the Ceramide Kinase Inhibitor K1, a Suppressor of Mast-Cell Activation

Hirotaka KUMADA; Susumu MITSUTAKE; Yuichi INAGAKI; Shino MITSUNAGA; Hiroshi TSUCHIKAWA; Shigeo KATSUMURA; Yasuyuki IGARASHI

doi:10.1271/bbb.70308

Biochemistry & Molecular Biology Notes

Kinetics of the Ceramide Kinase Inhibitor K1, a Suppressor of Mast-Cell Activation

Hirotaka KUMADA, Susumu MITSUTAKE, Yuichi INAGAKI, Shino MITSUNAGA, Hiroshi TSUCHIKAWA, Shigeo KATSUMURA, Yasuyuki IGARASHI

Author information

Hirotaka KUMADA
Laboratory of Biomembrane and Biofunctional Chemistry, Faculty of Pharmaceutical Science and Faculty of Advanced Life Sciences, Hokkaido University
Susumu MITSUTAKE
Laboratory of Biomembrane and Biofunctional Chemistry, Faculty of Pharmaceutical Science and Faculty of Advanced Life Sciences, Hokkaido University
Yuichi INAGAKI
Laboratory of Biomembrane and Biofunctional Chemistry, Faculty of Pharmaceutical Science and Faculty of Advanced Life Sciences, Hokkaido University
Shino MITSUNAGA
School of Science and Technology, Kwansei Gakuin University
Hiroshi TSUCHIKAWA
School of Science and Technology, Kwansei Gakuin University
Shigeo KATSUMURA
School of Science and Technology, Kwansei Gakuin University
Yasuyuki IGARASHI
Laboratory of Biomembrane and Biofunctional Chemistry, Faculty of Pharmaceutical Science and Faculty of Advanced Life Sciences, Hokkaido University

Keywords: ceramide, ceramide kinase, ceramide 1-phosphate, sphingolipid

JOURNAL FREE ACCESS

2007 Volume 71 Issue 10 Pages 2581-2584

DOI https://doi.org/10.1271/bbb.70308

View "Advance Publication" version (October 7, 2007).

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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.

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