Literature summary for 1.1.98.3 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.

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Cloned(Commentary)

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

Protein Variants

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

Inhibitors

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism	UniProt	Comment	Textmining
Mycobacterium tuberculosis	P9WJF1	-	-
Mycobacterium tuberculosis H37Rv	P9WJF1	-	-

Substrates and Products (Substrate)

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

Synonyms

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

Cofactor

Cofactor	Comment	Organism	Structure
FAD	-	Mycobacterium tuberculosis

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Release 2023.1 (January 2023)