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Literature summary for 2.1.1.374 extracted from

  • Warrier, T.; Kapilashrami, K.; Argyrou, A.; Ioerger, T.; Little, D.; Murphye, K.; Nandakumar, M.; Park, S.; Gold, B.; Mi, J.; Zhang, T.; Meiler, E.; Rees, M.; Somersan-Karakaya, S.; Francisco, E.; Martinez-Hoyos, M.; Burns-Huang, K.; Roberts, J.; Ling, Y.
    N-Methylation of a bactericidal compound as a resistance mechanism in Mycobacterium tuberculosis (2016), Proc. Natl. Acad. Sci. USA, 113, E4523-E4530 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.1.1.374

Protein Variants

Protein Variants Comment Organism
S140A increased methyltransferase activity of relative to wild-type enzyme Mycobacterium tuberculosis

Inhibitors

Inhibitors Comment Organism Structure
S-adenosyl-L-homocysteine
-
 Mycobacterium tuberculosis

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0014
-
 3-methyl-1-oxo-2-[3-oxo-3-(pyrrolidin-1-yl)propyl]-1,5-dihydrobenzo[4,5]imidazo[1,2-a]pyridine-4-carbonitrile pH 7.4, 37°C, mutant enzyme S140A Mycobacterium tuberculosis
0.004
-
 3-methyl-1-oxo-2-[3-oxo-3-(pyrrolidin-1-yl)propyl]-1,5-dihydrobenzo[4,5]imidazo[1,2-a]pyridine-4-carbonitrile pH 7.4, 37°C, wild-type enzyme Mycobacterium tuberculosis

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
S-adenosyl-L-methionine + 3-methyl-1-oxo-2-[3-oxo-3-(pyrrolidin-1-yl)propyl]-1,5-dihydrobenzo[4,5]imidazo[1,2-a]pyridine-4-carbonitrile Mycobacterium tuberculosis
-
 S-adenosyl-L-homocysteine + ?
-
 ?

Organism

Organism UniProt Comment Textmining
Mycobacterium tuberculosis
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
S-adenosyl-L-methionine + 3-methyl-1-oxo-2-[3-oxo-3-(pyrrolidin-1-yl)propyl]-1,5-dihydrobenzo[4,5]imidazo[1,2-a]pyridine-4-carbonitrile
-
 Mycobacterium tuberculosis S-adenosyl-L-homocysteine + ?
-
 ?

Synonyms

Synonyms Comment Organism
rv0560c
-
 Mycobacterium tuberculosis

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Mycobacterium tuberculosis

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.00123
-
 3-methyl-1-oxo-2-[3-oxo-3-(pyrrolidin-1-yl)propyl]-1,5-dihydrobenzo[4,5]imidazo[1,2-a]pyridine-4-carbonitrile pH 7.4, 37°C, wild-type enzyme Mycobacterium tuberculosis
0.0028
-
 3-methyl-1-oxo-2-[3-oxo-3-(pyrrolidin-1-yl)propyl]-1,5-dihydrobenzo[4,5]imidazo[1,2-a]pyridine-4-carbonitrile pH 7.4, 37°C, mutant enzyme S140A Mycobacterium tuberculosis

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
 assay at Mycobacterium tuberculosis

Expression

Organism Comment Expression
Mycobacterium tuberculosis clones bearing mutations in a transcription factor, Rv2887, markedly up-regulate the expression of rv0560c up

General Information

General Information Comment Organism
physiological function the enzyme N-methylates N-methylates the bactericidal compound 3-methyl-1-oxo-2-[3-oxo-3-(pyrrolidin-1-yl)propyl]-1,5-dihydrobenzo[4,5]imidazo[1,2-a]pyridine-4-carbonitrile, abrogating its bactericidal activity. Methylation of an antibacterial compound is a mode of antimicrobial resistance Mycobacterium tuberculosis

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
0.3075
-
 3-methyl-1-oxo-2-[3-oxo-3-(pyrrolidin-1-yl)propyl]-1,5-dihydrobenzo[4,5]imidazo[1,2-a]pyridine-4-carbonitrile pH 7.4, 37°C, wild-type enzyme Mycobacterium tuberculosis
2
-
 3-methyl-1-oxo-2-[3-oxo-3-(pyrrolidin-1-yl)propyl]-1,5-dihydrobenzo[4,5]imidazo[1,2-a]pyridine-4-carbonitrile pH 7.4, 37°C, mutant enzyme S140A Mycobacterium tuberculosis