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Literature summary extracted from

  • Foo, C.S.; Lechartier, B.; Kolly, G.S.; Boy-Roettger, S.; Neres, J.; Rybniker, J.; Lupien, A.; Sala, C.; Piton, J.; Cole, S.T.
    Characterization of DprE1-mediated benzothiazinone resistance in Mycobacterium tuberculosis (2016), Antimicrob. Agents Chemother., 60, 6451-6459.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.1.98.3 expressed in Escherichia coli BL21(DE3) cells Mycobacterium tuberculosis

Protein Variants

EC Number Protein Variants Comment Organism
1.1.98.3 C387A the mutation confers resistance to benzothiazinones Mycobacterium tuberculosis
1.1.98.3 C387G the mutation confers resistance to benzothiazinones and reduces the overall catalytic efficiency by about 4fold compared to the wild type enzyme Mycobacterium tuberculosis
1.1.98.3 C387N the mutation confers resistance to benzothiazinones and reduces the overall catalytic efficiency by about 4fold compared to the wild type enzyme Mycobacterium tuberculosis
1.1.98.3 C387S the mutation confers resistance to benzothiazinones Mycobacterium tuberculosis
1.1.98.3 C387T the mutation confers resistance to benzothiazinones Mycobacterium tuberculosis

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.98.3 2-[4-(cyclohexylmethyl)piperazin-1-yl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one complete inhibition at 0.04 mM Mycobacterium tuberculosis
1.1.98.3 3-{[(4-methoxyphenyl)methyl]amino}-6-(trifluoromethyl)quinoxaline-2-carboxylic acid 97% inhibition at 0.04 mM Mycobacterium tuberculosis
1.1.98.3 additional information not inhibited by rifampin Mycobacterium tuberculosis

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.1.98.3 trans,octacis-decaprenylphospho-beta-D-ribofuranose + FAD Mycobacterium tuberculosis
-
trans,octacis-decaprenylphospho-beta-D-erythro-pentofuranosid-2-ulose + FADH2
-
?
1.1.98.3 trans,octacis-decaprenylphospho-beta-D-ribofuranose + FAD Mycobacterium tuberculosis H37Rv
-
trans,octacis-decaprenylphospho-beta-D-erythro-pentofuranosid-2-ulose + FADH2
-
?

Organism

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

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.98.3 trans,octacis-decaprenylphospho-beta-D-ribofuranose + FAD
-
Mycobacterium tuberculosis trans,octacis-decaprenylphospho-beta-D-erythro-pentofuranosid-2-ulose + FADH2
-
?
1.1.98.3 trans,octacis-decaprenylphospho-beta-D-ribofuranose + FAD
-
Mycobacterium tuberculosis H37Rv trans,octacis-decaprenylphospho-beta-D-erythro-pentofuranosid-2-ulose + FADH2
-
?

Synonyms

EC Number Synonyms Comment Organism
1.1.98.3 decaprenylphosphoryl-beta-D-ribose oxidase
-
Mycobacterium tuberculosis
1.1.98.3 DprE1
-
Mycobacterium tuberculosis

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.98.3 FAD
-
Mycobacterium tuberculosis