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Literature summary extracted from

  • Madikane, V.E.; Bhakta, S.; Russell, A.J.; Campbell, W.E.; Claridge, T.D.; Elisha, B.G.; Davies, S.G.; Smith, P.; Sim, E.
    Inhibition of mycobacterial arylamine N-acetyltransferase contributes to anti-mycobacterial activity of Warburgia salutaris (2007), Bioorg. Med. Chem., 15, 3579-3586.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.3.1.5 drug development the enzyme is a target for development of anti-mycobacterial drugs Mycolicibacterium smegmatis
2.3.1.5 drug development the enzyme is a target for development of anti-mycobacterial drugs Mycobacterium tuberculosis
2.3.1.5 drug development the enzyme is a target for development of anti-mycobacterial drugs Mycobacterium tuberculosis variant bovis
2.3.1.5 medicine results show that Warburgia salutaris is a useful source of anti-tubercular compounds for further analysis and supports the hypothesis of a link between NAT inhibition and antimycobacterial activity Mycolicibacterium smegmatis
2.3.1.5 medicine results show that Warburgia salutaris is a useful source of anti-tubercular compounds for further analysis and supports the hypothesis of a link between NAT inhibition and antimycobacterial activity Mycobacterium tuberculosis variant bovis
2.3.1.5 medicine Warburgia salutaris is a useful source of anti-tubercular compounds for further analysis and supports the hypothesis of a link between NAT inhibition and anti-mycobacterial activity Mycolicibacterium smegmatis

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.3.1.5 expressed in Escherichia coli as a His-tagged fusion protein Mycolicibacterium smegmatis
2.3.1.5 expression of N-terminally His6-tagged NAT in Escherichia coli strain BL21(DE3) Mycolicibacterium smegmatis
2.3.1.5 the open-reading frame of the gene for Mycobacterium smegmatis N-acetyltransferase plus an N-terminal hexa-histidine tag is expressed in Escherichia coli BL21DE3-pLysS cells Mycolicibacterium smegmatis

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.5 11alpha-hydroxycinnamosmolide a drimane sesquiterpenoid lactone from Warburgia salutaris inhibits the purified mycobacterial enzyme and contributes to the anti-mycobacterial activity of Warburgia salutaris Mycobacterium tuberculosis
2.3.1.5 11alpha-hydroxycinnamosmolide a drimane sesquiterpenoid lactone from Warburgia salutaris inhibits the purified mycobacterial enzyme and contributes to the anti-mycobacterial activity of Warburgia salutaris, the component or extract has no effect on a Nat-deficient Mycobacterium bovis strain; a drimane sesquiterpenoid lactone isolated from Warburgia salutaris. Compound inhibits the growth of Mycobacterium bovis BCG wild-type in a dose-dependent fashion, while it had little effect of the growth of Mycobacterium bovis BCG nat deleted mutant Mycobacterium tuberculosis variant bovis
2.3.1.5 11alpha-hydroxycinnamosmolide a drimane sesquiterpenoid lactone from Warburgia salutaris inhibits the purified mycobacterial enzyme and contributes to the anti-mycobacterial activity of Warburgia salutaris, 35% inhibition of the recombinant enzyme at 0.5 mg/ml; a novel drimane sesquiterpenoid lactone isolated from Warburgia salutaris. Compound inhibits recombinant NAT activity of Mycobacterium smegmatis (35% inhibition of acetylation at 0.5 mg/mL). Compound exhibits anti-mycobacterial activity against Mycobacterium tuberculosis H37Rv and Mycobacterium bovis BCG Pasteur. Compound does not inhibit growth of Escherichia coli and is not toxic to cultured mammalian macrophage cells at the concentrations at which anti-mycobacterial activity is observed; isolated from the bark of Warburgia salutaris Mycolicibacterium smegmatis
2.3.1.5 Warburgia salutaris extract
-
 Mycolicibacterium smegmatis

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.3.1.5 acetyl-CoA + an arylamine Mycolicibacterium smegmatis
-
 CoA + an N-acetylarylamine
-
 ?
2.3.1.5 acetyl-CoA + an arylamine Mycobacterium tuberculosis
-
 CoA + an N-acetylarylamine
-
 ?
2.3.1.5 acetyl-CoA + an arylamine Mycobacterium tuberculosis variant bovis
-
 CoA + an N-acetylarylamine
-
 ?
2.3.1.5 acetyl-CoA + an arylamine Mycobacterium tuberculosis H37Rv
-
 CoA + an N-acetylarylamine
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.5 Mycobacterium tuberculosis
-
-
-
2.3.1.5 Mycobacterium tuberculosis H37Rv
-
-
-
2.3.1.5 Mycobacterium tuberculosis variant bovis
-
-
-
2.3.1.5 Mycobacterium tuberculosis variant bovis
-
 Pasteur
-
2.3.1.5 Mycolicibacterium smegmatis
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.3.1.5 recombinant N-terminally His6-tagged NAT from Escherichia coli strain BL21(DE3) by nickel affinity chromatography Mycolicibacterium smegmatis
2.3.1.5 using Ni-NTA agarose, the hexa-his-tag is removed by thrombin cleavage Mycolicibacterium smegmatis
2.3.1.5 using using Ni-NTA agarose Mycolicibacterium smegmatis

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.3.1.5 acetyl-CoA + an arylamine
-
 Mycolicibacterium smegmatis CoA + an N-acetylarylamine
-
 ?
2.3.1.5 acetyl-CoA + an arylamine
-
 Mycobacterium tuberculosis CoA + an N-acetylarylamine
-
 ?
2.3.1.5 acetyl-CoA + an arylamine
-
 Mycobacterium tuberculosis variant bovis CoA + an N-acetylarylamine
-
 ?
2.3.1.5 acetyl-CoA + an arylamine
-
 Mycobacterium tuberculosis H37Rv CoA + an N-acetylarylamine
-
 ?
2.3.1.5 acetyl-CoA + isoniazid
-
 Mycolicibacterium smegmatis CoA + N-acetyl-isoniazid
-
 ?
2.3.1.5 acetyl-CoA + isoniazid
-
 Mycobacterium tuberculosis variant bovis CoA + N-acetyl-isoniazid
-
 ?
2.3.1.5 acetyl-CoA + isoniazid
-
 Mycolicibacterium smegmatis ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.3.1.5 arylamine N-acetyltransferase
-
 Mycolicibacterium smegmatis
2.3.1.5 arylamine N-acetyltransferase
-
 Mycobacterium tuberculosis variant bovis
2.3.1.5 arylamine N-acetyltransferase C
-
 Mycolicibacterium smegmatis
2.3.1.5 MSNAT
-
 Mycolicibacterium smegmatis
2.3.1.5 NAT
-
 Mycolicibacterium smegmatis
2.3.1.5 NAT
-
 Mycobacterium tuberculosis
2.3.1.5 NAT
-
 Mycobacterium tuberculosis variant bovis

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.3.1.5 37
-
 assay at Mycolicibacterium smegmatis
2.3.1.5 37
-
 assay at Mycobacterium tuberculosis variant bovis
2.3.1.5 37
-
 activity assay Mycolicibacterium smegmatis

Cofactor

EC Number Cofactor Comment Organism Structure
2.3.1.5 acetyl-CoA
-
 Mycolicibacterium smegmatis
2.3.1.5 acetyl-CoA
-
 Mycobacterium tuberculosis
2.3.1.5 acetyl-CoA
-
 Mycobacterium tuberculosis variant bovis