Structure-activity relationship of okadaic acid, a potent protein phosphatases PP1 and PP2A inhibitor: 24-epi-okadaic acid and a 18-membered lactone analog

Masaki Kita, Makoto Kuramoto, Tatsuhiko Chiba, Akihiro Yamada, Nobuko Yamada, Takako Ishida, Takeharu Haino, Kaoru Yamada, Yasuharu Ijuin, Osamu Ohno, Daisuke Uemura

Research output: Contribution to journalArticle

6 Citations (Scopus)

Abstract

X-Ray crystallographic analysis and structure-activity relationship of okadaic acid revealed that the flexible cavity structure stabilized by intramolecular hydrogen bonds is important for its potent cytotoxicity.

Original languageEnglish
Pages (from-to)1033-1042
Number of pages10
JournalHeterocycles
Volume76
Issue number2
DOIs
Publication statusPublished - 2008 Nov 1

Keywords

  • 24-epi-OA
  • Flexible Cavity Structure
  • OA Lactone
  • Ocadaic Acid
  • Protein Phosphatase

ASJC Scopus subject areas

  • Analytical Chemistry
  • Pharmacology
  • Organic Chemistry

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    Kita, M., Kuramoto, M., Chiba, T., Yamada, A., Yamada, N., Ishida, T., Haino, T., Yamada, K., Ijuin, Y., Ohno, O., & Uemura, D. (2008). Structure-activity relationship of okadaic acid, a potent protein phosphatases PP1 and PP2A inhibitor: 24-epi-okadaic acid and a 18-membered lactone analog. Heterocycles, 76(2), 1033-1042. https://doi.org/10.3987/COM-08-S(N)88