Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
1-(isonicotinamido)-N2,N4-bis(benzo[d]thiazol-2-yl)azetidine-2,4-dicarboxamide
1-(isonicotinamido)-N2,N4-bis(phenyl)azetidine-2,4-dicarboxamide
lead compound for inhibitor screening, involved in hydrophobic interactions with residues Pro242, Val241, Ala176, Leu130, Ile267, Ala179, Ile199 and Ile174
2,4,6-Trinitrobenzenesulfonic acid
-
inactivation follows pseudo first-order kinetics with a 1:1 stoichiometric ratio between the reagent and the enzyme subunit. Partial protection by each of the substrates, NADH or pyruvate. Complete protection only in presence of the ternary complex enzyme-NADH-pyruvate
2-ethyl-N-phenethyl-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-amine
the molecule shows activity against nutrient-starved nonreplicating Mycobacterium tuberculosis, resulting in a 2.7 log reduction of bacterial loads at 0.010 mg/ml, and is shown to be more potent than the first-line antitubercular drugs, isoniazid and rifampicin, at the same dose. compound is cytotoxic
-
3-(2-pyridyldithio)propionate
-
inactivation follows pseudo first-order kinetics with a 1:1 stoichiometric ratio between the reagent and the enzyme subunit. Partial protection by each of the substrates, NADH or pyruvate. Complete protection only in presence of the ternary complex enzyme-NADH-pyruvate
3-hydroxypyruvate
-
competitive with respect to pyruvate
4-(furan-2-ylmethylene)-1-phenylpyrazolidine-3,5-dione
the compound exhibited potent antitubercular activity against log-phase cultures of Mycobacterium tuberculosis with a MIC of 0.0245 mM, but is found to be less active than the lead compound 1-(4-chlorophenyl)-4-(4-hydroxy-3-methoxy-5-nitrobenzylidene) pyrazolidine-3,5-dione (CD59). The compound is cytotoxic
-
5'-(p-(fluorosulfonyl)-benzoyl)adenosine
-
inactivation follows pseudo-first-order kinetics, complete inactivation of the enzyme can not be obtained even at high reagent concentration
5,5'-dithiobis(2-nitrobenzoate)
-
-
5-(4-(benzyloxy)benzylidene)-3-(2,5-dimethylphenyl)-2-iminothiazolidin-4-one
compound shows potency, selectivity, and no cytotoxicity up to 50 microM in a mouse macrophage cell line
5-(4-(benzyloxy)benzylidene)-3-(2,6-dimethylphenyl)-2-iminothiazolidin-4-one
compound shows potency, selectivity, and no cytotoxicity up to 50 microM in a mouse macrophage cell line
6-acetyl-2-(4-chlorobenzamido)-4,5,6,7-tetrahydrothieno[2,3-c]pyridine-3-carboxamide
compound shows potency, selectivity, and no cytotoxicity up to 50 microM in a mouse macrophage cell line
AgNO3
-
0.1 mM, 57% inhibition
Ca2+
Alkalihalophilus pseudofirmus
80% inhibition at 10 mM, 71% at 1 mM, 21% at 0.1 mM
Cibacron blue F3GA
0.1 mM, 70% inhibition
D-alanine
AlaDH enzyme activity is completely inhibited by D-alanine in a competitive manner
DTNB
7% inhibition with 0.01 M and 40% inhibition with 0.1 mM
DTT
Alkalihalophilus pseudofirmus
39% inhibition at 10 mM
Fe3+
-
10 mM, 85% inhibition of reductive amination
KCl
slightly enhances PvRA activity and it moderately promotes ALD activity. In contrast, increasing amounts of KCl gradually inhibits GxRA activity
L-alanine
the PvRA activity of ApAlaDH is strongly inhibited by 2 mM L-alanine, 68% inhibition. The GxRA activity is completely inhibited in the presence of L-alanine (100% inhibition at 10 and 20 mM L-alanine)
L-Phe
-
reductive amination of pyruvate, 10 mM, 28% inhibition
L-Trp
-
reductive amination of pyruvate, 10 mM, 29% inhibition
methyl p-nitrobenzenesulfonate
0.1 mM, complete inhibition
MnSO4
-
10 mM, 50% inhibition
NaCl
NaCl does not inhibit PvRA activity up to 1 M, but inhibition is observed at 2.5 M. The activities of ALD and GxRA are significantly increased in the presence of NaCl at concentrations of 0.1-0.25 M
NADPH
-
inhibition of reductive amination
Ni2+
-
10 mM, 60% inhibition of reductive amination
p-hydroxymercuribenzoate
-
no effect on aminating activity, inhibition of deaminating activity
pyridoxal 5'-phosphate
-
-
tert-butyl 3-carbamoyl-2-(4-chlorobenzamido)-4,5-dihydrothieno[2,3-c]pyridine-6(7H)-carboxylate
compound shows potency, selectivity, and no cytotoxicity up to 50 microM in a mouse macrophage cell line
1-(isonicotinamido)-N2,N4-bis(benzo[d]thiazol-2-yl)azetidine-2,4-dicarboxamide
compound shows 100fold reduction in nutrient starved dormant Mycobacterium tuberculosis model and MIC of 11.81 microM in actively replicative Mycobacterium tuberculosis
1-(isonicotinamido)-N2,N4-bis(benzo[d]thiazol-2-yl)azetidine-2,4-dicarboxamide
-
CaCl2
-
10 mM, 22% inhibition
CaCl2
1 mM, 15% inhibition
Cd2+
-
10 mM, 36% inhibition of reductive amination
Cibacron blue
-
-
Co2+
Alkalihalophilus pseudofirmus
complete inhibition at 10 mM, 27% at 0.1 mM
Co2+
-
10 mM, 60% inhibition of reductive amination
Co2+
-
17% inhibition at 10 mM, 23.75% at 20 mM
CoCl2
-
0.1 mM, 53% inhibition
Cu2+
Alkalihalophilus pseudofirmus
complete inhibition at 10 mM, 34% at 0.1 mM
Cu2+
-
10 mM, 60% inhibition of reductive amination
CuCl2
-
1 mM, 52% inhibition
CuSO4
-
10 mM, 36% inhibition
CuSO4
-
50.7% inhibition by 1 mM, 96.3% inhibition by 20 mM, EDTA in a 10fold molar excess restores activity almost completely, recombinant enzyme
D-Ala
-
-
D-Ala
-
aminating reaction, competitive with respect to NADH, noncompetitive with respect to NH4+ and pyruvate
D-Cys
-
-
EDTA
Alkalihalophilus pseudofirmus
34% inhibition at 10 mM
Fe2+
-
10 mM, 85% inhibition of reductive amination
glycine
-
-
glycine
GxRA activity is inhibited by 60% in presence of 20 mM glycine, but glycine does not inhibit the PvRA activity
Hg2+
-
-
HgCl2
-
0.003 mM, complete inhibition
HgCl2
-
1 mM, 38% inhibition
HgCl2
complete inhibition
HgCl2
1 mM, complete inhibition
Hydroxypyruvate
-
-
iodoacetate
-
-
iodoacetate
-
23.75% inhibition at 10 mM
L-Ala
-
-
L-Ala
-
reductive amination of pyruvate
L-Ala
-
uncompetitive inhibition with respect to NADH
L-Ala
-
substrate inhibition
L-Ala
-
5 mM, 34% inhibition
L-Ala
-
reductive amination of pyruvate
L-Cys
-
-
L-Cys
10 mM, 40% inhibition
L-Ser
-
-
L-Ser
-
inhibition of aminating activity
L-Ser
-
inhibition of aminating activity
L-Ser
-
reductive amination of pyruvate
L-Ser
-
10 mM, 26% inhibition; inhibition of aminating activity
L-Ser
-
inhibition of aminating activity
L-Thr
-
inhibition of aminating activity
L-Thr
-
reductive amination of pyruvate, 10 mM, 37% inhibition
Mercurials
-
-
-
MgCl2
-
inhibitory at a concentration above 2.13 mM
Mn2+
Alkalihalophilus pseudofirmus
complete inhibition at 10 mM, 25% at 1 mM
Mn2+
-
10 mM, 60% inhibition of reductive amination
MnCl2
-
10 mM, 12% inhibition
MnCl2
1 mM, 10% inhibition
NAD+
-
product inhibition
NAD+
-
0.1 mM, 35% inhibition
NADH
-
-
NADH
-
product inhibition
NADH
-
product inhibition
NH4+
-
-
NH4+
-
product inhibition
NH4+
-
inhibition of aminating activity
Pb2+
Alkalihalophilus pseudofirmus
protein OF4Ald completely loses its activity in the presence of 0.1-10 mM Pb2+
PCMB
-
-
PCMB
-
0.3 mM, 52% inhibition
PCMB
0.1 mM, 97% inhibition
pyruvate
the ALD activity of ApAlaDH is strongly inhibited by 2 mM L-alanine, 45% inhibition
pyruvate
-
product inhibition
pyruvate
-
substrate inhibition
pyruvate
-
inhibition at pH 7.5 greater than at pH 9.5; product inhibition
pyruvate
-
substrate inhibition
pyruvate
-
product inhibition
Zn2+
-
-
Zn2+
-
10 mM, 62% inhibition
Zn2+
-
allosteric competitive inhibitor, reversible, inducing conformational change through the intersubunit interaction, positive cooperative binding of the substrate in presence of Zn2+
Zn2+
-
26.5% inhibition by 1 mM ZnCl2, 90.1% inhibition by 20 mM ZnCl2, EDTA in a 10fold molar excess restores activity almost completely, recombinant enzyme
Zn2+
-
57% inhibition at 10 mM, 72.75% at 20 mM
additional information
all enzyme reactions are inhibited to varying degrees by their products
-
additional information
-
all enzyme reactions are inhibited to varying degrees by their products
-
additional information
development and optimization of compounds that inhibits the enzyme and can act as anti-tuberculosis drug, overview
-
additional information
-
development and optimization of compounds that inhibits the enzyme and can act as anti-tuberculosis drug, overview
-
additional information
no inhibition by L-serine and L-valine
-