Carvalho, Mariele C.; Tomazini, Atilio; Prado, Rogilene A.; Viviani, Vadim R. published the artcile< Selective inhibition of Zophobas morio (Coleoptera: Tenebrionidae) luciferase-like enzyme luminescence by diclofenac and potential suitability for light-off biosensing>, Application In Synthesis of 2591-17-5, the main research area is diclofenac; luciferase-like enzyme; luminescence; toxicity.
The accumulation of toxic carboxylic compounds may cause severe effects on the environment and living organisms. A luciferase-like enzyme, previously cloned from the Malpighian tubules of the non-luminescent Zophobas morio mealworm, displays thioesterification activity with a wide range of carboxylic substrates, and produces weak red luminescence in the presence of ATP and firefly -luciferin, a xenobiotic for this organism. To better investigate the function of this enzyme in carboxylic xenobiotic detoxification, we analyzed the inhibitory effect of different xenobiotic carboxylic acids on the luminescence activity of this enzyme, including environmental pollutants and pharmaceutical compounds Noteworthy, the anti-inflammatory drug diclofenac severely inhibited this luciferase-like enzyme luminescence activity, both in in vitro (IC50 20 μM) and in vivo in bacterial cells assays, when compared with other beetle luciferases. Similar results were obtained with its brighter I327S mutant. Kinetic anal. of diclofenac′s effect on luminescence activity indicated mixed-type inhibition for both ATP and -luciferin. Modeling studies showed five potential binding sites for diclofenac, including the CoA binding site, which showed one of the highest binding constant Taken together, these results raise the possibility of using this luciferase-like enzyme for the development of novel whole-cell luminescent biosensors for diclofenac and similar drugs.
Luminescence published new progress about 2591-17-5. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Application In Synthesis of 2591-17-5.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica