Design and synthesis of AX7574: A microcystin-derived, fluorescent probe for serine/threonine phosphatases

被引：39

作者：

Shreder, KR ^{[1
]}

Liu, YS ^{[1
]}

Nomanhboy, T ^{[1
]}

Fuller, SR ^{[1
]}

Wong, MS ^{[1
]}

Gai, WZ ^{[1
]}

Wu, JY ^{[1
]}

Leventhal, PS ^{[1
]}

Lill, JR ^{[1
]}

Corral, S ^{[1
]}

机构：

[1] ActivX Biosci Inc, La Jolla, CA 92037 USA

来源：

BIOCONJUGATE CHEMISTRY | 2004年 / 15卷 / 04期

关键词：

D O I：

10.1021/bc0499580

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

The design and synthesis of AX7574, a microcystin-derived probe for serine/threonine phosphatases, is described. A key step in the synthesis was the conjugation under basic conditions of a tetramethylrhodamine 1,3-diketone derivative to the arginine side chain present in microcystin-LR. The resulting conjugate specifically labeled the active site of protein phosphatases 1 (PP-1) with a 1:1 stoichiometry and IC50 of 4.0 nM. AX7574 was used to isolate and identify PP-1, PP-2A, PP-4, and PP-6 in Jurkat cells. Finally, AX7574 was able to record changes in the phosphatase activity levels of calyculin A treated Jurkat cells versus untreated control cells.

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收藏

页码：790 / 798

页数：9

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