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An electrophoretic mobility shift assay for the identification and kinetic analysis of acetyl transferase inhibitors |
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| Authors: | Caroline Fanslau Sujatha Nagulapalli Suhong Pang Jonathan Lippy |
| Institution: | a Mechanistic Biochemistry, Bristol-Myers Squibb, Princeton, NJ 08543, USA b Discovery Biology, Bristol-Myers Squibb, Princeton, NJ 08543, USA c Lead Evaluation, Bristol-Myers Squibb, Princeton, NJ 08543, USA |
| Abstract: | Histone acetyl transferases are important regulators of cellular homeostasis. This study describes a sensitive acetyl transferase electrophoretic mobility shift assay applicable both for kinetic analysis of acetyl transferase inhibitors and for high-throughput testing. Application of the assay for human GCN5L2 enabled dissection of inhibitor competition with respect to acetyl coenzyme A. Furthermore, we demonstrated that the assay can detect time-dependent inhibition of human GCN5L2 by reactive inhibitors. |
| Keywords: | Electrophoretic mobility shift assay Acetyl transferase GCN5 |
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