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SLAS Discov 24(7):745-754, 745-754. Evaluation of Luminogenic Substrates as Probe Substrates for Bacterial Cytochrome P450 Enzymes: Application to Mycobacterium tuberculosis. 2019

Ortega Ugalde, S., Ma, D., Cali, J.J., and Commandeur, J.N.M.

Notes: Pro-luciferin substrates were evaluated as substrates for Mycobacterium tuberculosis cytochrome P450 enzymes to support applicability for high-throughput screening. (5206)

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J. Pharmacol. Toxicol. Methods 92, 77-94. mRNA transfection retrofits cell-based assays with xenobiotic metabolism. 2018

DeGroot, D.E., Swank, A., Thomas, R.S., Strynar, M., Lee, M.Y., Carmichael, P.L., and Simmons, S.O.

Notes: The ten most common human liver cytochrome P450 enzymes were introduced into a HEK293T cell line to support the creation of high throughput screening assays. Luminogenic substrates for the P450 enzymes were used to assess activity. (5212)

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Expert Opin. Drug Metab. Toxicol. 4, 103–120. Bioluminescent assays for ADMET 2008

Cali, J.J., Niles, A., Valley, M.P., O’Brien, M.A., Riss, T.L., and Shultz, J.

Notes: The authors of this review article highlight the use of bioluminescence as a readout for high-throughput ADME/Tox assays. They discuss three strategies for designing bioluminescent assays, using either luciferase, ATP or luciferin substrates as the limiting reagents for a luciferase-catalyzed reaction. Reporter gene assays limit the production of luciferase by tying it to a promoter or DNA regulatory region of interest. Such assays can be used to study genes that are regulated by drugs and other xenobiotics. Bioluminescent assays in which ATP is the limiting reagent of the luciferase reaction can be designed to monitor cell viability or the activity kinases. Bioluminescent assays in which the substrate is limiting can be designed so that the activity of a particular enzyme results in the production of a luciferin substrate that can, in turn, be acted upon by luciferase. (3926)

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