17(ß-Hydroxy-16α-[125I]iodowortmannin, a sensitive labeling agent for pi 3-kinases

Shinobu Honzawa, Hiroshi Kurosu, Osamu Hazeki, Toshiaki Katada, Masakatsu Shibasaki, Masahisa Nakada

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

To detect phosphatidylinositol (PI) 3-kinases with high sensitivity, we designed and prepared a radiolabeled derivative of wortmannin (1), a potent inhibitor of PI 3-kinases. The synthesized derivative, 17ß-hydroxy-16α-[125I]iodowortmannin (7), showed an IC50 that was 100-fold higher than that of wortmannin itself and which bound to catalytic subunits of PI 3-kinases.

Original languageEnglish
Pages (from-to)2276-2278
Number of pages3
JournalChemical and Pharmaceutical Bulletin
Volume43
Issue number12
DOIs
Publication statusPublished - 1995 Jan 1

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Keywords

  • PI 3-kinase
  • radiolabeling
  • signal transduction
  • wortmannin

ASJC Scopus subject areas

  • Chemistry(all)
  • Drug Discovery

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