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Literature summary for 4.1.1.48 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

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

Cloned(Commentary)

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

Protein Variants

Protein Variants Comment Organism
E168A site directed mutagenesis Mycobacterium tuberculosis
E168A site directed mutagenesis Mycobacterium tuberculosis H37Ra
H170A site directed mutagenesis Mycobacterium tuberculosis
H170A site directed mutagenesis Mycobacterium tuberculosis H37Ra
L193A site directed mutagenesis Mycobacterium tuberculosis
L193A site directed mutagenesis Mycobacterium tuberculosis H37Ra
L196A site directed mutagenesis Mycobacterium tuberculosis
L196A site directed mutagenesis Mycobacterium tuberculosis H37Ra
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
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
N189A site directed mutagenesis Mycobacterium tuberculosis
N189A site directed mutagenesis Mycobacterium tuberculosis H37Ra
N192A site directed mutagenesis Mycobacterium tuberculosis
N192A site directed mutagenesis Mycobacterium tuberculosis H37Ra
P63A site directed mutagenesis Mycobacterium tuberculosis
P63A site directed mutagenesis Mycobacterium tuberculosis H37Ra
R191A site directed mutagenesis Mycobacterium tuberculosis
R191A site directed mutagenesis Mycobacterium tuberculosis H37Ra
S64A site directed mutagenesis Mycobacterium tuberculosis
S64A site directed mutagenesis Mycobacterium tuberculosis H37Ra
V169A site directed mutagenesis Mycobacterium tuberculosis
V169A site directed mutagenesis Mycobacterium tuberculosis H37Ra

Inhibitors

Inhibitors Comment Organism Structure
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
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
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
L-tryptophan tryptophan at high concentrations has definite inhibitory activity against Mycobacterium tuberculosis but does not antagonize the activity of ATB107 Mycobacterium tuberculosis
additional information inhibitory effect of ATB107 can not be reversed by the addition of tryptophan Mycobacterium tuberculosis
additional information inhibitory effect of ATB107 can not be reversed by the addition of tryptophan Mycobacterium tuberculosis H37Ra
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]

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

Organism

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

Substrates and Products (Substrate)

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

Subunits

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

Synonyms

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