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Literature summary for 2.5.1.78 extracted from

  • Cushman, M.; Yang, D.; Mihalic, J.T.; Chen, J.; Gerhardt, S.; Huber, R.; Fischer, M.; Kis, K.; Bacher, A.
    Incorporation of an amide into 5-phosphonoalkyl-6-D-ribitylaminopyrimidinedione lumazine synthase inhibitors results in an unexpected reversal of selectivity for riboflavin synthase vs lumazine synthase (2002), J. Org. Chem., 67, 6871-6877.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression of beta60 capsid carying lumazine synthase activity Bacillus subtilis

Inhibitors

Inhibitors Comment Organism Structure
5-(4-phosphonobutyryl)amino-6-D-ribitylaminouracil comparison with inhibition of Escherichia coli riboflavin synthase Bacillus subtilis
5-(5-phosphonopentyl)amino-6-D-ribitylaminouracil comparison with inhibition of Escherichia coli riboflavin synthase Bacillus subtilis
5-(5-phosphonoxyvaleryl)amino-6-D-ribitylaminouracil mixed inhibition, comparison with inhibition of Escherichia coli riboflavin synthase Bacillus subtilis
5-(hexyl 6-dihydrogen phosphate)-6-([(2S,3S,4R)-2,3,4,5-tetrahydroxypentyl]amino)pyrimidine-2,4(1H,3H)-dione mixed inhibition, comparison with inhibition of Escherichia coli riboflavin synthase Bacillus subtilis
additional information incorporation of an amide into 5-phosphonoalkyl-6-D-ribitylaminopyrimidinedione lumazine synthase inhibitors results in an unexpected reversal of selectivity for riboflavin synthase versus lumazine synthase Bacillus subtilis

Organism

Organism UniProt Comment Textmining
Bacillus subtilis
-
lumazine synthase/riboflavin synthase complex
-

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Bacillus subtilis

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Bacillus subtilis

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.13
-
5-(hexyl 6-dihydrogen phosphate)-6-([(2S,3S,4R)-2,3,4,5-tetrahydroxypentyl]amino)pyrimidine-2,4(1H,3H)-dione pH 7.5, 37°C, recombinant beta60 capsid Bacillus subtilis
0.83
-
5-(5-phosphonoxyvaleryl)amino-6-D-ribitylaminouracil pH 7.5, 37°C, recombinant beta60 capsid Bacillus subtilis
0.86
-
5-(4-phosphonobutyryl)amino-6-D-ribitylaminouracil pH 7.5, 37°C, recombinant beta60 capsid Bacillus subtilis
1
-
5-(5-phosphonopentyl)amino-6-D-ribitylaminouracil pH 7.5, 37°C, recombinant beta60 capsid Bacillus subtilis