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Literature summary extracted from

  • Trefzer, C.; Rengifo-Gonzalez, M.; Hinner, M.J.; Schneider, P.; Makarov, V.; Cole, S.T.; Johnsson, K.
    Benzothiazinones: prodrugs that covalently modify the decaprenylphosphoryl-beta-D-ribose 2-epimerase DprE1 of Mycobacterium tuberculosis (2010), J. Am. Chem. Soc., 132, 13663-13665.
    View publication on PubMed

Protein Variants

EC Number Protein Variants Comment Organism
1.1.98.3 C387G mutation confers resistance to 1-methyl-2,4,7-trinitroxanthone and to 3-nitro-N-[(1R)-1-phenylethyl]-5-(trifluoromethyl)benzamide Mycobacterium tuberculosis
1.1.98.3 C387S mutation confers resistance to 1-methyl-2,4,7-trinitroxanthone and to 3-nitro-N-[(1R)-1-phenylethyl]-5-(trifluoromethyl)benzamide Mycobacterium tuberculosis

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.98.3 1-methyl-2,4,7-trinitroxanthone mutations C387S and C387G confer resistance to 1-methyl-2,4,7-trinitroxanthone Mycobacterium tuberculosis
1.1.98.3 2-[(2S)-2-methyl-1,4-dioxa-8-azaspiro[4.5]dec-8-yl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one tuberculosis drug candidate with high activity against Mycobacterium tuberculosis in vitro and in vivo. Compound is activated in the bacterium by reduction of an essential nitro group to a nitroso derivative, which then specifically reacts with a cysteine residue in the active site of DprE1 Mycobacterium tuberculosis
1.1.98.3 3-nitro-N-[(1R)-1-phenylethyl]-5-(trifluoromethyl)benzamide high activity against Mycobacterium smegmatis and Mycobacterium tuberculosis H37Rv but no significant activity against benzothiazinone-resistant strains with the mutations Cys387Ser or Cys387Gly in DprE1 Mycobacterium tuberculosis

Organism

EC Number Organism UniProt Comment Textmining
1.1.98.3 Mycobacterium tuberculosis P9WJF1
-
-
1.1.98.3 Mycobacterium tuberculosis H37Rv P9WJF1
-
-

Synonyms

EC Number Synonyms Comment Organism
1.1.98.3 DprE1
-
Mycobacterium tuberculosis