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

Fingerprint

Okadaic Acid
Phosphoprotein Phosphatases
Lactones
Structure-Activity Relationship
Cytotoxicity
Hydrogen
Hydrogen bonds
X-Rays
X rays

Keywords

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

ASJC Scopus subject areas

  • Analytical Chemistry
  • Organic Chemistry
  • Pharmacology

Cite this

Structure-activity relationship of okadaic acid, a potent protein phosphatases PP1 and PP2A inhibitor : 24-epi-okadaic acid and a 18-membered lactone analog. / Kita, Masaki; Kuramoto, Makoto; Chiba, Tatsuhiko; Yamada, Akihiro; Yamada, Nobuko; Ishida, Takako; Haino, Takeharu; Yamada, Kaoru; Ijuin, Yasuharu; Ohno, Osamu; Uemura, Daisuke.

In: Heterocycles, Vol. 76, No. 2, 01.11.2008, p. 1033-1042.

Research output: Contribution to journalArticle

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, vol. 76, no. 2, pp. 1033-1042. https://doi.org/10.3987/COM-08-S(N)88
Kita, Masaki ; Kuramoto, Makoto ; Chiba, Tatsuhiko ; Yamada, Akihiro ; Yamada, Nobuko ; Ishida, Takako ; Haino, Takeharu ; Yamada, Kaoru ; Ijuin, Yasuharu ; Ohno, Osamu ; Uemura, Daisuke. / Structure-activity relationship of okadaic acid, a potent protein phosphatases PP1 and PP2A inhibitor : 24-epi-okadaic acid and a 18-membered lactone analog. In: Heterocycles. 2008 ; Vol. 76, No. 2. pp. 1033-1042.
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