Identification of a molecular target of kurahyne, an apoptosis-inducing lipopeptide from marine cyanobacterial assemblages

[Display omitted] In 2014, we isolated kurahyne, an acetylene-containing lipopeptide, from a marine cyanobacterial assemblage of Lyngbya sp. Kurahyne exhibited growth-inhibitory activity against human cancer cells, and induced apoptosis in HeLa cells. However, its mode of action is not yet clear. To...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2015-11, Vol.25 (22), p.5295-5298
Hauptverfasser: Iwasaki, Arihiro, Ohno, Osamu, Katsuyama, Shun, Morita, Maho, Sasazawa, Yukiko, Dan, Shingo, Simizu, Siro, Yamori, Takao, Suenaga, Kiyotake
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Sprache:eng
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Zusammenfassung:[Display omitted] In 2014, we isolated kurahyne, an acetylene-containing lipopeptide, from a marine cyanobacterial assemblage of Lyngbya sp. Kurahyne exhibited growth-inhibitory activity against human cancer cells, and induced apoptosis in HeLa cells. However, its mode of action is not yet clear. To elucidate its mode of action, we carried out several cell-based assays, and identified the intracellular target molecule of kurahyne as sarco/endoplasmic reticulum Ca2+ ATPase (SERCA). In addition, we found that kurahyne inhibited the differentiation of macrophages into osteoclasts.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2015.09.044