Artificial ladder-shaped polyethers that inhibit maitotoxin-induced Ca2+ influx in rat glioma C6 cells

Bioorg Med Chem Lett. 2012 Jun 1;22(11):3619-22. doi: 10.1016/j.bmcl.2012.04.053.

Tohru Oishi ¹, Keiichi Konoki, Rie Tamate, Kohei Torikai, Futoshi Hasegawa, Nobuaki Matsumori, Michio Murata

Affiliations

Affiliation

1 Department of Chemistry, Faculty and Graduate School of Sciences, Kyushu University, Higashi-ku, Fukuoka, Japan. [email protected]

PMID: 22560474 DOI: 10.1016/j.bmcl.2012.04.053

Abstract

Maitotoxin (MTX) is a ladder-shaped polyether produced by the epiphytic dinoflagellate Gambierdiscus toxicus. It is known to elicit potent toxicity against mammals and induce influx of CA(2+) into cells. An artificial ladder-shaped polyether possessing a 6/7/6/6/7/6/6 heptacyclic ring system, which was designed for elucidating interactions with transmembrane proteins, was found to be the most potent inhibitor against MTX-induced CA(2+) influx that has ever been reported.

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