Interferences with Luciferase Reporter Enzymes
- PMID: 27478246
- Bookshelf ID: NBK374281
Interferences with Luciferase Reporter Enzymes
Excerpt
Here we describe the molecular basis underlying interference by inhibitors of reporter enzymes for biochemical and cell-based assays. This understanding is used to create strategies to mitigate the confounding effects reporter enzyme inhibitor interference has on interpreting high throughput screening results, and to aid in evaluating chemical probes derived from reporter gene assays. As well, example compounds that act as potent inhibitors of luciferases are described which can serve as useful tools when developing luciferase-based assays.
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References
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- Fersht A. Enzyme Structure and Mechanism. 2nd Edition. . W.H. Freeman and Company.; 1984. p. 176.
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- Dahlin JL, Baell J, Walters MA. Assay Interference by Chemical Reactivity: NCBI; 2015 [Sep. 18 2015]. Available from: http://www.ncbi.nlm.nih.gov/books/NBK53196/.
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- Simeonov A, Davis MI. Interference with Fluorescence and Absorbance: NCBI; 2015 [December 7, 2015]. Available from: http://www.ncbi.nlm.nih.gov/books/NBK53196/.
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- Thorne N, Shen M, Lea WA, Simeonov A, Lovell S, Auld DS, Inglese J. Firefly luciferase in chemical biology: a compendium of inhibitors, mechanistic evaluation of chemotypes, and suggested use as a reporter. Chem Biol. 2012;19(8):1060–72. doi: 10.1016/j.chembiol.2012.07.015. Epub 2012/08/28. doiPMCID: 3449281. - DOI - PMC - PubMed
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