| Autor: |
Shreder KR; ActivX Biosciences, Inc., 11025 N. Torrey Pines Road; La Jolla, California 92037, USA. kevins@activx.com, Liu Y, Nomanhboy T, Fuller SR, Wong MS, Gai WZ, Wu J, Leventhal PS, Lill JR, Corral S |
| Jazyk: |
angličtina |
| Zdroj: |
Bioconjugate chemistry [Bioconjug Chem] 2004 Jul-Aug; Vol. 15 (4), pp. 790-8. |
| DOI: |
10.1021/bc0499580 |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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