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Issue 3, 2014
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Cysteine-reactive chemical probes based on a modular 4-aminopiperidine scaffold

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Abstract

We utilized tri-functionalized 4-aminopiperidine as a modular scaffold to generate a cysteine-reactive probe library. Using in-gel fluorescence screening against lysates overexpressing glutathione S-transferase omega 1 (GSTO1) and the protein kinase AKT1, we identified SMC-1 and SMC-8 as activity-dependent covalent modifiers of these enzymes. These compounds are ideal chemical probes to monitor enzyme activity in proteomes.

Graphical abstract: Cysteine-reactive chemical probes based on a modular 4-aminopiperidine scaffold

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Article information


Submitted
01 Oct 2013
Accepted
09 Oct 2013
First published
15 Oct 2013

Med. Chem. Commun., 2014,5, 358-362
Article type
Concise Article

Cysteine-reactive chemical probes based on a modular 4-aminopiperidine scaffold

S. M. Couvertier and E. Weerapana, Med. Chem. Commun., 2014, 5, 358
DOI: 10.1039/C3MD00289F

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