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Literature summary for 2.3.1.5 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

Application Comment Organism
drug development the enzyme is a target for development of anti-mycobacterial drugs Mycolicibacterium smegmatis
drug development the enzyme is a target for development of anti-mycobacterial drugs Mycobacterium tuberculosis
drug development the enzyme is a target for development of anti-mycobacterial drugs Mycobacterium tuberculosis variant bovis
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
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
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)

Cloned (Comment) Organism
expressed in Escherichia coli as a His-tagged fusion protein Mycolicibacterium smegmatis
expression of N-terminally His6-tagged NAT in Escherichia coli strain BL21(DE3) Mycolicibacterium smegmatis
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

Inhibitors Comment Organism Structure
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
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
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
Warburgia salutaris extract
-
Mycolicibacterium smegmatis

Natural Substrates/ Products (Substrates)

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

Organism

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

Purification (Commentary)

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

Substrates and Products (Substrate)

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

Synonyms

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

Temperature Optimum [°C]

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

Cofactor

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