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

doi:10.1248/cpb.43.2276

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

^*Corresponding author for this work

School of Advanced Science and Engineering

Research output: Contribution to journal › Article › peer-review

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 language	English
Pages (from-to)	2276-2278
Number of pages	3
Journal	Chemical and Pharmaceutical Bulletin
Volume	43
Issue number	12
DOIs	https://doi.org/10.1248/cpb.43.2276
Publication status	Published - 1995

Keywords

PI 3-kinase
radiolabeling
signal transduction
wortmannin

ASJC Scopus subject areas

Chemistry(all)
Drug Discovery

Access to Document

10.1248/cpb.43.2276

Cite this

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title = "17({\ss}-Hydroxy-16α-[125I]iodowortmannin, a sensitive labeling agent for pi 3-kinases",

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, 17{\ss}-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.",

keywords = "PI 3-kinase, radiolabeling, signal transduction, wortmannin",

author = "Shinobu Honzawa and Hiroshi Kurosu and Osamu Hazeki and Toshiaki Katada and Masakatsu Shibasaki and Masahisa Nakada",

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T1 - 17(ß-Hydroxy-16α-[125I]iodowortmannin, a sensitive labeling agent for pi 3-kinases

AU - Honzawa, Shinobu

AU - Kurosu, Hiroshi

AU - Hazeki, Osamu

AU - Katada, Toshiaki

AU - Shibasaki, Masakatsu

AU - Nakada, Masahisa

PY - 1995

Y1 - 1995

N2 - 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.

AB - 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.

KW - PI 3-kinase

KW - radiolabeling

KW - signal transduction

KW - wortmannin

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