Biselyngbyasides, cytotoxic marine macrolides, are novel and potent inhibitors of the Ca2+ pumps with a unique mode of binding

Maho Morita, Haruo Ogawa, Osamu Ohno, Takao Yamori, Kiyotake Suenaga, Chikashi Toyoshima

研究成果: Article査読

18 被引用数 (Scopus)

抄録

Biselyngbyasides (BLSs), macrolides from a marine cyanobacterium, are cytotoxic natural products whose target molecule is unknown. Here we report that BLSs are high affinity (Ki ∼ 10 nM) inhibitors of Ca2+-pumps with a unique binding mode. The crystal structures of the Ca2+-pump in complex with BLSs at 3.2-3.5 Å-resolution show that BLSs bind to the pump near the cytoplasmic surface of the transmembrane region. The crystal structures and activity measurement of BLS analogs allow us to identify the structural features that confer high potency to BLSs as inhibitors of the pump.

本文言語English
ページ(範囲)1406-1411
ページ数6
ジャーナルFEBS Letters
589
13
DOI
出版ステータスPublished - 2015 5 26

ASJC Scopus subject areas

  • 生物理学
  • 構造生物学
  • 生化学
  • 分子生物学
  • 遺伝学
  • 細胞生物学

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