A Rapidly Reversible Chemical Dimerizer System to Study Lipid Signaling in Living Cells1. Issue 26 (19th May 2014)

• Record Type: Journal Article
• Authors: Feng, Suihan; Laketa, Vibor; Stein, Frank; Rutkowska, Anna; MacNamara, Aidan; Depner, Sofia; Klingmüller, Ursula; Saez‐Rodriguez, Julio; Schultz, Carsten
• Is Part Of: Angewandte Chemie international edition. Volume 53:Issue 26(2014)
• Page Start: 6720
• Page End: 6723
• Publication Date: 2014-05-19
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1002/anie.201402294
• Languages: English
• ISSNs: 1433-7851

Abstract

<abstract abstract-type="main" xml:lang="en"> <title>Abstract</title> <p>Chemical dimerizers are powerful tools for non‐invasive manipulation of enzyme activities in intact cells. Here we introduce the first rapidly reversible small‐molecule‐based dimerization system and demonstrate a sufficiently fast switch‐off to determine kinetics of lipid metabolizing enzymes in living cells. We applied this new method to induce and stop phosphatidylinositol 3‐kinase (PI3K) activity, allowing us to quantitatively measure the turnover of phosphatidylinositol 3, 4, 5‐trisphosphate (PIP₃) and its downstream effectors by confocal fluorescence microscopy as well as standard biochemical methods.</p> </abstract>