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Literature summary extracted from

  • Shen, H.; Wang, F.; Zhang, Y.; Huang, Q.; Xu, S.; Hu, H.; Yue, J.; Wang, H.
    A novel inhibitor of indole-3-glycerol phosphate synthase with activity against multidrug-resistant Mycobacterium tuberculosis (2009), FEBS J., 276, 144-154.
    View publication on PubMed

Application

EC Number Application Comment Organism
4.1.1.48 medicine IGPS may be a potential target for the development of anti-tuberculosis drugs Mycobacterium tuberculosis
4.1.1.48 medicine IGPS may be a potential target for the development of anti-tuberculosis drugs Mycobacterium tuberculosis variant bovis BCG
4.1.1.48 medicine IGPS may be a potential target for the development of anti-tuberculosis drugs Mycobacterium tuberculosis H37Ra

Cloned(Commentary)

EC Number Cloned (Comment) Organism
4.1.1.48 expressed in Escherichia coli strain BL21 Mycobacterium tuberculosis
4.1.1.48 expressed in Escherichia coli strain BL21 Mycobacterium tuberculosis H37Ra

Protein Variants

EC Number Protein Variants Comment Organism
4.1.1.48 E168A site directed mutagenesis Mycobacterium tuberculosis
4.1.1.48 E168A site directed mutagenesis Mycobacterium tuberculosis H37Ra
4.1.1.48 H170A site directed mutagenesis Mycobacterium tuberculosis
4.1.1.48 H170A site directed mutagenesis Mycobacterium tuberculosis H37Ra
4.1.1.48 L193A site directed mutagenesis Mycobacterium tuberculosis
4.1.1.48 L193A site directed mutagenesis Mycobacterium tuberculosis H37Ra
4.1.1.48 L196A site directed mutagenesis Mycobacterium tuberculosis
4.1.1.48 L196A site directed mutagenesis Mycobacterium tuberculosis H37Ra
4.1.1.48 additional information site directed mutagenesis studies indicate that ATB107 may inhibit IGPS activity by reducing the binding affinity for substrate of residues Glu168 and Asn189 Mycobacterium tuberculosis
4.1.1.48 additional information site directed mutagenesis studies indicate that ATB107 may inhibit IGPS activity by reducing the binding affinity for substrate of residues Glu168 and Asn189 Mycobacterium tuberculosis H37Ra
4.1.1.48 N189A site directed mutagenesis Mycobacterium tuberculosis
4.1.1.48 N189A site directed mutagenesis Mycobacterium tuberculosis H37Ra
4.1.1.48 N192A site directed mutagenesis Mycobacterium tuberculosis
4.1.1.48 N192A site directed mutagenesis Mycobacterium tuberculosis H37Ra
4.1.1.48 P63A site directed mutagenesis Mycobacterium tuberculosis
4.1.1.48 P63A site directed mutagenesis Mycobacterium tuberculosis H37Ra
4.1.1.48 R191A site directed mutagenesis Mycobacterium tuberculosis
4.1.1.48 R191A site directed mutagenesis Mycobacterium tuberculosis H37Ra
4.1.1.48 S64A site directed mutagenesis Mycobacterium tuberculosis
4.1.1.48 S64A site directed mutagenesis Mycobacterium tuberculosis H37Ra
4.1.1.48 V169A site directed mutagenesis Mycobacterium tuberculosis
4.1.1.48 V169A site directed mutagenesis Mycobacterium tuberculosis H37Ra

Inhibitors

EC Number Inhibitors Comment Organism Structure
4.1.1.48 ATB107 1-azabicyclo[2.2.2]octan-3-one[4-(phenylamino)-6-(1-piperidinyl)-1,3,5-triazin-2-yl]hydrazone, 0.1 microg/ml minimum inhibitory concentration, potent competitive inhibitor of the substrate 1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate Mycobacterium tuberculosis
4.1.1.48 ATB107 1-azabicyclo[2.2.2]octan-3-one[4-(phenylamino)-6-(1-piperidinyl)-1,3,5-triazin-2-yl]hydrazone, 0.1 microg/ml minimum inhibitory concentration, potent competitive inhibitor of the substrate 1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate Mycobacterium tuberculosis H37Ra
4.1.1.48 ATB107 1-azabicyclo[2.2.2]octan-3-one[4-(phenylamino)-6-(1-piperidinyl)-1,3,5-triazin-2-yl]hydrazone, 0.1 microg/ml minimum inhibitory concentration, potent competitive inhibitor of the substrate 1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate Mycobacterium tuberculosis variant bovis BCG
4.1.1.48 L-tryptophan tryptophan at high concentrations has definite inhibitory activity against Mycobacterium tuberculosis but does not antagonize the activity of ATB107 Mycobacterium tuberculosis
4.1.1.48 additional information inhibitory effect of ATB107 can not be reversed by the addition of tryptophan Mycobacterium tuberculosis
4.1.1.48 additional information inhibitory effect of ATB107 can not be reversed by the addition of tryptophan Mycobacterium tuberculosis H37Ra
4.1.1.48 tryptophan tryptophan at high concentrations has definite inhibitory activity against Mycobacterium tuberculosis but does not antagonize the activity of ATB107 Mycobacterium tuberculosis H37Ra

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
4.1.1.48 1.13
-
1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate increased Km value in the presence of ATB107 Mycobacterium tuberculosis
4.1.1.48 1.13
-
1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate increased Km value in the presence of ATB107 Mycobacterium tuberculosis H37Ra
4.1.1.48 1.19
-
1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate H170A site directed mutagenesis Mycobacterium tuberculosis
4.1.1.48 1.19
-
1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate H170A site directed mutagenesis Mycobacterium tuberculosis H37Ra
4.1.1.48 1.42
-
1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate L193A site directed mutagenesis Mycobacterium tuberculosis
4.1.1.48 1.42
-
1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate L193A site directed mutagenesis Mycobacterium tuberculosis H37Ra
4.1.1.48 1.53
-
1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate S64A site directed mutagenesis Mycobacterium tuberculosis
4.1.1.48 1.53
-
1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate S64A site directed mutagenesis Mycobacterium tuberculosis H37Ra
4.1.1.48 1.53
-
1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate V169A site directed mutagenesis Mycobacterium tuberculosis
4.1.1.48 1.53
-
1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate V169A site directed mutagenesis Mycobacterium tuberculosis H37Ra
4.1.1.48 1.81
-
1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate L196A site directed mutagenesis Mycobacterium tuberculosis
4.1.1.48 1.81
-
1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate L196A site directed mutagenesis Mycobacterium tuberculosis H37Ra
4.1.1.48 2.49
-
1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate P63A site directed mutagenesis Mycobacterium tuberculosis
4.1.1.48 2.49
-
1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate P63A site directed mutagenesis Mycobacterium tuberculosis H37Ra
4.1.1.48 2.57
-
1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate N192A site directed mutagenesis Mycobacterium tuberculosis
4.1.1.48 2.57
-
1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate N192A site directed mutagenesis Mycobacterium tuberculosis H37Ra
4.1.1.48 6.63
-
1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate R191A site directed mutagenesis Mycobacterium tuberculosis
4.1.1.48 6.63
-
1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate R191A site directed mutagenesis Mycobacterium tuberculosis H37Ra
4.1.1.48 20.34
-
1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate N189A site directed mutagenesis Mycobacterium tuberculosis
4.1.1.48 20.34
-
1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate N189A site directed mutagenesis Mycobacterium tuberculosis H37Ra
4.1.1.48 21.67
-
1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate E168A site directed mutagenesis Mycobacterium tuberculosis
4.1.1.48 21.67
-
1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate E168A site directed mutagenesis Mycobacterium tuberculosis H37Ra

Organism

EC Number Organism UniProt Comment Textmining
4.1.1.48 Mycobacterium tuberculosis P9WFX7
-
-
4.1.1.48 Mycobacterium tuberculosis H37Ra A5U2W7
-
-
4.1.1.48 Mycobacterium tuberculosis H37Rv P9WFX7
-
-
4.1.1.48 Mycobacterium tuberculosis variant bovis BCG A1KJ27
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4.1.1.48 1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate + ?
-
Mycobacterium tuberculosis 1-C-(indol-3-yl)glycerol 3-phosphate + CO2 + H2O
-
?
4.1.1.48 1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate + ?
-
Mycobacterium tuberculosis variant bovis BCG 1-C-(indol-3-yl)glycerol 3-phosphate + CO2 + H2O
-
?
4.1.1.48 1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate + ?
-
Mycobacterium tuberculosis H37Ra 1-C-(indol-3-yl)glycerol 3-phosphate + CO2 + H2O
-
?
4.1.1.48 1-(2-carboxyphenylamino)-1-deoxy-D-ribulose-5-phosphate + ?
-
Mycobacterium tuberculosis H37Rv 1-C-(indol-3-yl)glycerol 3-phosphate + CO2 + H2O
-
?

Subunits

EC Number Subunits Comment Organism
4.1.1.48 More one typical (beta /alpha)8-barrel structure Mycobacterium tuberculosis
4.1.1.48 More one typical (beta /alpha)8-barrel structure Mycobacterium tuberculosis H37Ra

Synonyms

EC Number Synonyms Comment Organism
4.1.1.48 IGPS
-
Mycobacterium tuberculosis
4.1.1.48 IGPS
-
Mycobacterium tuberculosis variant bovis BCG
4.1.1.48 IGPS
-
Mycobacterium tuberculosis H37Ra
4.1.1.48 indole-3-glycerol phosphate synthase
-
Mycobacterium tuberculosis
4.1.1.48 indole-3-glycerol phosphate synthase
-
Mycobacterium tuberculosis variant bovis BCG
4.1.1.48 indole-3-glycerol phosphate synthase
-
Mycobacterium tuberculosis H37Ra
4.1.1.48 mIGPS
-
Mycobacterium tuberculosis
4.1.1.48 mIGPS
-
Mycobacterium tuberculosis variant bovis BCG
4.1.1.48 mIGPS
-
Mycobacterium tuberculosis H37Ra