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Paper | Special issue | Vol 79, No. 1, 2009, pp.1007-1017
Published online, 12th December, 2008
DOI: 10.3987/COM-08-S(D)78
Maitotoxin-Photoactive Probe Binds to Membrane Proteins in Blood Cells

Keiichi Konoki,* Masaki Hashimoto, Kaori Honda, Kazuo Tachibana, Rie Tamate, Futoshi Hasegawa, Tohru Oishi, and Michio Murata*

*Department of Chemistry, Faculty of Science, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan


The photoactive and biotinylating ligand was prepared from MTX and maleimide-conjugated Hatanaka reagent with use of Diels-Alder reaction. Blood cells were subjected to affinity labelling experiments using the ligand thus obtained. The labelled band on SDS-PAGE was replaced not by MTX but by brevetoxin B (PbTx2), which suggested the presence of binding proteins in blood cells. Screening of polyether compounds for MTX inhibitory activity using Ca2+ flux assays in C6 cells disclosed that a synthetic fragment of the hydrophilic portion of MTX inhibited the MTX activity.