A high-throughput screening platform for inhibitors of the riboflavin biosynthesis pathway

作者：Kaiser Johannes; Illarionov Boris; Rohdich Felix; Eisenreich Wolfgang; Saller Sabine; Van den Brulle Jan; Cushman Mark; Bacher Adelbert; Fischer Markus^*

来源：Analytical Biochemistry, 2007, 365(1): 52-61.

DOI：10.1016/j.ab.2007.02.033

• riboflavin biosynthesis
• 3,4-dihydroxy-2-butanone 4-phosphate synthase
• 6,7-dimethyl-8-ribityllumazine synthase
• riboflavin synthase
• high-throughput screening for inhibitors
• targets for novel antiinfective drugs

3,4-Dihydroxy-2-butanone 4-phosphate synthase, 6,7-dimethyl-8-ribityllumazine synthase, and riboflavin synthase of the riboflavin biosynthetic pathway are potential targets for novel antiinfective drugs. This article describes a platform for high-throughput screening for inhibitors of these enzymes. The assays can be monitored photometrically and have been shown to be robust, as indicated by Z factors >= 0.87. A C-13 NMR assay for hit verification of 3,4-dihydroxy-2-butanone 4-phosphate synthase inhibitors is also reported.

• 出版日期2007-6-1