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Literature summary extracted from

  • Makowska-Grzyska, M.; Kim, Y.; Maltseva, N.; Osipiuk, J.; Gu, M.; Zhang, M.; Mandapati, K.; Gollapalli, D.R.; Gorla, S.K.; Hedstrom, L.; Joachimiak, A.
    A novel cofactor-binding mode in bacterial IMP dehydrogenases explains inhibitor selectivity (2015), J. Biol. Chem., 290, 5893-5911.
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
1.1.1.205 medicine MPDH inhibitors are used as immunosuppressive, antiviral, and anticancer agents Clostridium perfringens
1.1.1.205 medicine MPDH inhibitors are used as immunosuppressive, antiviral, and anticancer agents Vibrio cholerae serotype O1
1.1.1.205 medicine MPDH inhibitors are used as immunosuppressive, antiviral, and anticancer agents Campylobacter jejuni
1.1.1.205 medicine MPDH inhibitors are used as immunosuppressive, antiviral, and anticancer agents Bacillus anthracis

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.1.1.205 gene impdh, sequence comparisons, recombinant expression of N-terminally His-tagged long and short enzyme CBS-deletion mutants, BaIMPDHDELTAL and BaIMPDHDELTAS, in Escherichia coli Bacillus anthracis
1.1.1.205 gene impdh, sequence comparisons, recombinant expression of N-terminally His-tagged long enzyme CBS-deletion mutant, ClpIMPDHDELTAL, in Escherichia coli Clostridium perfringens
1.1.1.205 gene impdh, sequence comparisons, recombinant expression of N-terminally His-tagged long enzyme CBS-deletion mutant, VcIMPDHDELTAL, in Escherichia coli Vibrio cholerae serotype O1
1.1.1.205 gene impdh, sequence comparisons, recombinant expression of N-terminally His-tagged short enzyme CBS-deletion mutant, CjIMPDHDELTAS, in Escherichia coli Campylobacter jejuni

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
1.1.1.205 purified recombinant long enzyme mutant ClpIMPDHDELTAL in complex with IMP and with inhibitor 1 from 5% tacsimate, pH 7.0, 0.1 M HEPES, pH 7.0, 10% PEG MME 5000, 16°C, or with inhibitor 2 from 0.1 M ammonium acetate, 0.1 M Bis-Tris, pH 5.5, 17% PEG 10000, 16°C, X-ray diffraction structure determination and analysis at resolutions of 2.95 and 2.85 A, respectively Clostridium perfringens
1.1.1.205 purified recombinant long enzyme mutant VcIMPDHDELTAL in complex with IMP and NAD+ from 0.77 M sodium/potassium phosphate, 0.15 M Tris-HCl, pH 8.0, 6% MPD, 16°C, followed by soaking with 200 mM NAD+ solution for 15 min at 20°C, or enzyme mutant VcIMPDHDELTAL in complex with XMP and NADH from 1.03 M sodium/potassium phosphate, pH 5.0, 0.15 M sodium malate, 3% PEG 300, 16°C, followed by soaking with 200 mM NAD+ solution for 5 days at 16°C, X-ray diffraction structure determination and analysis at resolutions of 2.38 and 1.66 A, respectively Vibrio cholerae serotype O1
1.1.1.205 purified recombinant short enzyme mutant BaIMPDHDELTAS in apoform from 0.2 M sodium chloride, 0.1 M sodium cacodylate, pH 6.5, and 2 M ammonium sulfate, 16°C, and purified recombinant long enzyme mutant BaIMPDHDELTAL in complex with IMP and with inhibitors 4-[(1R)-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4yl]ethoxy]quinoline-1-oxide, ((alpha-methyl-)N-2-naphthalenyl-2-(2-pyridinyl)-1H-benzimidazole-)1-acetamide, 3,4-dihydro-3-methyl-4-oxo-N-(6,7,8,9-tetrahydro2-dibenzofuranyl)-1-phthalazineacetamide, 2-chloro-N-methyl-5-[[[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]amino]carbonyl]aminobenzamide, N-(4-bromophenyl)-N-[1-[3-[1-(hydroxyimino)ethyl]phenyl]-1-methylethyl] urea, and 2-(1-naphthalenyloxy)-N-[(2-(4-pyridinyl)-5-benzoxazolyl)]-(2S)-propanamide in several conformations and under different conditions resulting in 6 different crystal structures, X-ray diffraction structure determination and analysis at resolutions of 1.93-2.85 A, respectively, overview Bacillus anthracis
1.1.1.205 purified recombinant short enzyme mutant CjIMPDHDELTAS in complex with IMP and with inhibitor 2 from 1.6 M ammonium sulfate, 0.1 M MES, pH 6.5, 10% dioxane, 16 °C, or with inhibitor 4 from 0.2 M lithium sulfate, 0.1 M CAPS, pH 10.5, 1.2 M sodium/0.8 M potassium phosphate, 16 °C, X-ray diffraction structure determination and analysis at resolutions of 2.44 and 2.54 A, respectively Campylobacter jejuni

Protein Variants

EC Number Protein Variants Comment Organism
1.1.1.205 additional information construction of a long CBS domain deletion mutant variant, ClpIMPDHDELTAL. Deletion of residues Gln89-Arg215 Clostridium perfringens
1.1.1.205 additional information construction of a long CBS domain deletion mutant variant, VcIMPDHDELTAL. Deletion of residues Phe91-Arg219 Vibrio cholerae serotype O1
1.1.1.205 additional information construction of a short and a long CBS domain deletion mutant variant, BaIMPDHDELTAS and BaIMPDHDELTAL. Deletion of residues Val95-Thr200 and Glu92-Arg220, respectively Bacillus anthracis
1.1.1.205 additional information construction of a short CBS domain deletion mutant variant, CjIMPDHDELTAS. Deletion of residues Val92-Thr195 Campylobacter jejuni

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.205 2-(1-naphthalenyloxy)-N-[(2-(4-pyridinyl)-5-benzoxazolyl)]-(2S)-propanamide
-
 Bacillus anthracis
1.1.1.205 2-(1-naphthalenyloxy)-N-[(2-(4-pyridinyl)-5-benzoxazolyl)]-(2S)-propanamide
-
 Campylobacter jejuni
1.1.1.205 2-(1-naphthalenyloxy)-N-[(2-(4-pyridinyl)-5-benzoxazolyl)]-(2S)-propanamide
-
 Clostridium perfringens
1.1.1.205 2-(1-naphthalenyloxy)-N-[(2-(4-pyridinyl)-5-benzoxazolyl)]-(2S)-propanamide
-
 Vibrio cholerae serotype O1
1.1.1.205 2-chloro-N-methyl-5-[[[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]amino]carbonyl]aminobenzamide
-
 Bacillus anthracis
1.1.1.205 2-chloro-N-methyl-5-[[[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]amino]carbonyl]aminobenzamide
-
 Campylobacter jejuni
1.1.1.205 2-chloro-N-methyl-5-[[[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]amino]carbonyl]aminobenzamide
-
 Clostridium perfringens
1.1.1.205 2-chloro-N-methyl-5-[[[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]amino]carbonyl]aminobenzamide
-
 Vibrio cholerae serotype O1
1.1.1.205 3,4-dihydro-3-methyl-4-oxo-N-(6,7,8,9-tetrahydro2-dibenzofuranyl)-1-phthalazineacetamide
-
 Bacillus anthracis
1.1.1.205 3,4-dihydro-3-methyl-4-oxo-N-(6,7,8,9-tetrahydro2-dibenzofuranyl)-1-phthalazineacetamide
-
 Campylobacter jejuni
1.1.1.205 3,4-dihydro-3-methyl-4-oxo-N-(6,7,8,9-tetrahydro2-dibenzofuranyl)-1-phthalazineacetamide
-
 Clostridium perfringens
1.1.1.205 3,4-dihydro-3-methyl-4-oxo-N-(6,7,8,9-tetrahydro2-dibenzofuranyl)-1-phthalazineacetamide
-
 Vibrio cholerae serotype O1
1.1.1.205 4-[(1R)-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4yl]ethoxy]quinoline-1-oxide
-
 Bacillus anthracis
1.1.1.205 4-[(1R)-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4yl]ethoxy]quinoline-1-oxide
-
 Campylobacter jejuni
1.1.1.205 4-[(1R)-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4yl]ethoxy]quinoline-1-oxide
-
 Clostridium perfringens
1.1.1.205 4-[(1R)-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4yl]ethoxy]quinoline-1-oxide
-
 Vibrio cholerae serotype O1
1.1.1.205 additional information inhibitor synthesis and binding structure to the enzyme determined with the CBS deletion mutant enzyme variants, overview Bacillus anthracis
1.1.1.205 additional information inhibitor synthesis and binding structure to the enzyme determined with the CBS deletion mutant enzyme variant, overview Campylobacter jejuni
1.1.1.205 additional information inhibitor synthesis and binding structure to the enzyme determined with the CBS deletion mutant enzyme variant, overview Clostridium perfringens
1.1.1.205 additional information inhibitor synthesis, overview Vibrio cholerae serotype O1
1.1.1.205 N-(4-bromophenyl)-N-[(1-methylethenyl)phenyl]ethyl urea
-
 Bacillus anthracis
1.1.1.205 N-(4-bromophenyl)-N-[(1-methylethenyl)phenyl]ethyl urea
-
 Campylobacter jejuni
1.1.1.205 N-(4-bromophenyl)-N-[(1-methylethenyl)phenyl]ethyl urea
-
 Clostridium perfringens
1.1.1.205 N-(4-bromophenyl)-N-[(1-methylethenyl)phenyl]ethyl urea
-
 Vibrio cholerae serotype O1
1.1.1.205 N-(4-bromophenyl)-N-[1-[3-[1-(hydroxyimino)ethyl]phenyl]-1-methylethyl] urea
-
 Bacillus anthracis
1.1.1.205 N-(4-bromophenyl)-N-[1-[3-[1-(hydroxyimino)ethyl]phenyl]-1-methylethyl] urea
-
 Campylobacter jejuni
1.1.1.205 N-(4-bromophenyl)-N-[1-[3-[1-(hydroxyimino)ethyl]phenyl]-1-methylethyl] urea
-
 Clostridium perfringens
1.1.1.205 N-(4-bromophenyl)-N-[1-[3-[1-(hydroxyimino)ethyl]phenyl]-1-methylethyl] urea
-
 Vibrio cholerae serotype O1
1.1.1.205 N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
-
 Bacillus anthracis
1.1.1.205 N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
-
 Campylobacter jejuni
1.1.1.205 N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
-
 Clostridium perfringens
1.1.1.205 N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
-
 Vibrio cholerae serotype O1
1.1.1.205 NAD+ substrate inhibition Bacillus anthracis
1.1.1.205 NAD+ substrate inhibition Campylobacter jejuni
1.1.1.205 NAD+ substrate inhibition Clostridium perfringens
1.1.1.205 NAD+ substrate inhibition Vibrio cholerae serotype O1

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.1.1.205 0.027
-
 IMP pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant CjIMPDHDELTAS Campylobacter jejuni
1.1.1.205 0.049
-
 IMP pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant ClpIMPDHDELTAL Clostridium perfringens
1.1.1.205 0.055
-
 IMP pH 8.0, 25°C, recombinant wild-type enzyme Campylobacter jejuni
1.1.1.205 0.061
-
 IMP pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant BaIMPDHDELTAS Bacillus anthracis
1.1.1.205 0.064
-
 IMP pH 8.0, 25°C, recombinant wild-type enzyme Bacillus anthracis
1.1.1.205 0.08
-
 IMP pH 8.0, 25°C, recombinant wild-type enzyme Vibrio cholerae serotype O1
1.1.1.205 0.087
-
 IMP pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant VcIMPDHDELTAL Vibrio cholerae serotype O1
1.1.1.205 0.1
-
 IMP pH 8.0, 25°C, recombinant wild-type enzyme Clostridium perfringens
1.1.1.205 0.15
-
 IMP pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant BaIMPDHDELTAL Bacillus anthracis
1.1.1.205 0.22
-
 NAD+ pH 8.0, 25°C, recombinant wild-type enzyme Campylobacter jejuni
1.1.1.205 0.37
-
 NAD+ pH 8.0, 25°C, recombinant wild-type enzyme Clostridium perfringens
1.1.1.205 0.46
-
 NAD+ pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant BaIMPDHDELTAL Bacillus anthracis
1.1.1.205 0.51
-
 NAD+ pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant ClpIMPDHDELTAL Clostridium perfringens
1.1.1.205 0.52
-
 NAD+ pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant CjIMPDHDELTAS Campylobacter jejuni
1.1.1.205 0.55
-
 NAD+ pH 8.0, 25°C, recombinant wild-type enzyme Bacillus anthracis
1.1.1.205 0.56
-
 NAD+ pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant BaIMPDHDELTAS Bacillus anthracis
1.1.1.205 1.1
-
 NAD+ pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant VcIMPDHDELTAL Vibrio cholerae serotype O1
1.1.1.205 1.2
-
 NAD+ pH 8.0, 25°C, recombinant wild-type enzyme Vibrio cholerae serotype O1

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
1.1.1.205 51943
-
-
 Vibrio cholerae serotype O1
1.1.1.205 52093
-
-
 Clostridium perfringens
1.1.1.205 52151
-
-
 Campylobacter jejuni
1.1.1.205 52374
-
-
 Bacillus anthracis

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.1.1.205 IMP + NAD+ + H2O Clostridium perfringens
-
 XMP + NADH + H+
-
 ?
1.1.1.205 IMP + NAD+ + H2O Vibrio cholerae serotype O1
-
 XMP + NADH + H+
-
 ?
1.1.1.205 IMP + NAD+ + H2O Campylobacter jejuni
-
 XMP + NADH + H+
-
 ?
1.1.1.205 IMP + NAD+ + H2O Bacillus anthracis
-
 XMP + NADH + H+
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.205 Bacillus anthracis
-
-
-
1.1.1.205 Campylobacter jejuni
-
-
-
1.1.1.205 Clostridium perfringens
-
-
-
1.1.1.205 Vibrio cholerae serotype O1
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.1.1.205 recombinant His-tagged long and short enzyme CBS-deletion mutants, BaIMPDHDELTAL and BaIMPDHDELTAS, from Escherichia coli by nickel affinity chromatography , tag cleavage by TEV protease, and removal by another step of nickel affinity chromatography, followed by dialysis Bacillus anthracis
1.1.1.205 recombinant His-tagged long enzyme CBS-deletion mutant, ClpIMPDHDELTAL, from Escherichia coli by nickel affinity chromatography , tag cleavage by TEV protease, and removal by another step of nickel affinity chromatography, followed by dialysis Clostridium perfringens
1.1.1.205 recombinant His-tagged long enzyme CBS-deletion mutant, VcIMPDHDELTAL, from Escherichia coli by nickel affinity chromatography , tag cleavage by TEV protease, and removal by another step of nickel affinity chromatography, followed by dialysis Vibrio cholerae serotype O1
1.1.1.205 recombinant His-tagged short enzyme CBS-deletion mutant, CjIMPDHDELTAS, from Escherichia coli by nickel affinity chromatography , tag cleavage by TEV protease, and removal by another step of nickel affinity chromatography, followed by dialysis Campylobacter jejuni

Reaction

EC Number Reaction Comment Organism Reaction ID
1.1.1.205 IMP + NAD+ + H2O = XMP + NADH + H+ the IMPDH reaction involves two chemical transformations. First, the catalytic Cys attacks IMP, and hydride is transferred to NAD to form the covalent intermediate E-XMP*. In the second step, E-XMP* is hydrolyzed to produce XMP Clostridium perfringens
a
1.1.1.205 IMP + NAD+ + H2O = XMP + NADH + H+ the IMPDH reaction involves two chemical transformations. First, the catalytic Cys attacks IMP, and hydride is transferred to NAD to form the covalent intermediate E-XMP*. In the second step, E-XMP* is hydrolyzed to produce XMP Vibrio cholerae serotype O1
a
1.1.1.205 IMP + NAD+ + H2O = XMP + NADH + H+ the IMPDH reaction involves two chemical transformations. First, the catalytic Cys attacks IMP, and hydride is transferred to NAD to form the covalent intermediate E-XMP*. In the second step, E-XMP* is hydrolyzed to produce XMP Campylobacter jejuni
a
1.1.1.205 IMP + NAD+ + H2O = XMP + NADH + H+ the IMPDH reaction involves two chemical transformations. First, the catalytic Cys attacks IMP, and hydride is transferred to NAD to form the covalent intermediate E-XMP*. In the second step, E-XMP* is hydrolyzed to produce XMP Bacillus anthracis
a

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.205 IMP + NAD+ + H2O
-
 Clostridium perfringens XMP + NADH + H+
-
 ?
1.1.1.205 IMP + NAD+ + H2O
-
 Vibrio cholerae serotype O1 XMP + NADH + H+
-
 ?
1.1.1.205 IMP + NAD+ + H2O
-
 Campylobacter jejuni XMP + NADH + H+
-
 ?
1.1.1.205 IMP + NAD+ + H2O
-
 Bacillus anthracis XMP + NADH + H+
-
 ?
1.1.1.205 additional information IMP- and XMP-enzyme binding structure analysis, overview Vibrio cholerae serotype O1 ?
-
 ?
1.1.1.205 additional information IMP-enzyme binding structure analysis, overview Clostridium perfringens ?
-
 ?
1.1.1.205 additional information IMP-enzyme binding structure analysis, overview Campylobacter jejuni ?
-
 ?
1.1.1.205 additional information IMP-enzyme binding structure analysis, overview Bacillus anthracis ?
-
 ?

Subunits

EC Number Subunits Comment Organism
1.1.1.205 tetramer 4 * 37929, long enzyme truncation CBS-mutant VcIMPDHDELTAL, sequence calculation Vibrio cholerae serotype O1
1.1.1.205 tetramer 4 * 38123, long enzyme truncation CBS-mutant ClpIMPDHDELTAL, sequence calculation Clostridium perfringens
1.1.1.205 tetramer 4 * 40435, long enzyme truncation CBS-mutant BaIMPDHDELTAL, sequence calculation, 4 * 37920, short enzyme truncation CBS-mutant BaIMPDHDELTAL, sequence calculation Bacillus anthracis
1.1.1.205 tetramer 4 * 40722, short enzyme truncation CBS-mutant CjIMPDHDELTAS, sequence calculation Campylobacter jejuni

Synonyms

EC Number Synonyms Comment Organism
1.1.1.205 IMP dehydrogenase
-
 Clostridium perfringens
1.1.1.205 IMP dehydrogenase
-
 Vibrio cholerae serotype O1
1.1.1.205 IMP dehydrogenase
-
 Campylobacter jejuni
1.1.1.205 IMP dehydrogenase
-
 Bacillus anthracis
1.1.1.205 IMPDH
-
 Clostridium perfringens
1.1.1.205 IMPDH
-
 Vibrio cholerae serotype O1
1.1.1.205 IMPDH
-
 Campylobacter jejuni
1.1.1.205 IMPDH
-
 Bacillus anthracis

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
1.1.1.205 25
-
 assay at Clostridium perfringens
1.1.1.205 25
-
 assay at Vibrio cholerae serotype O1
1.1.1.205 25
-
 assay at Campylobacter jejuni
1.1.1.205 25
-
 assay at Bacillus anthracis

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
1.1.1.205 1.8
-
 IMP pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant ClpIMPDHDELTAL Clostridium perfringens
1.1.1.205 1.9
-
 IMP pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant CjIMPDHDELTAS Campylobacter jejuni
1.1.1.205 2.1
-
 IMP pH 8.0, 25°C, recombinant wild-type enzyme Vibrio cholerae serotype O1
1.1.1.205 2.2
-
 IMP pH 8.0, 25°C, recombinant wild-type enzyme Campylobacter jejuni
1.1.1.205 2.9
-
 IMP pH 8.0, 25°C, recombinant wild-type enzyme Clostridium perfringens
1.1.1.205 4.5
-
 IMP pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant BaIMPDHDELTAL Bacillus anthracis
1.1.1.205 5.2
-
 IMP pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant VcIMPDHDELTAL Vibrio cholerae serotype O1
1.1.1.205 5.3
-
 IMP pH 8.0, 25°C, recombinant wild-type enzyme Bacillus anthracis
1.1.1.205 6.1
-
 IMP pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant BaIMPDHDELTAS Bacillus anthracis

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.1.1.205 8
-
 assay at Clostridium perfringens
1.1.1.205 8
-
 assay at Vibrio cholerae serotype O1
1.1.1.205 8
-
 assay at Campylobacter jejuni
1.1.1.205 8
-
 assay at Bacillus anthracis

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.205 NAD+ enzyme binding structure analysis, overview Clostridium perfringens
1.1.1.205 NAD+ enzyme binding structure analysis, overview Vibrio cholerae serotype O1
1.1.1.205 NAD+ enzyme binding structure analysis, overview Campylobacter jejuni
1.1.1.205 NAD+ enzyme binding structure analysis, overview Bacillus anthracis

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.1.1.205 3.8
-
 NAD+ pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant BaIMPDHDELTAL Bacillus anthracis
1.1.1.205 3.9
-
 NAD+ pH 8.0, 25°C, recombinant wild-type enzyme Bacillus anthracis
1.1.1.205 5.3
-
 NAD+ pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant BaIMPDHDELTAS Bacillus anthracis
1.1.1.205 6.4
-
 NAD+ pH 8.0, 25°C, recombinant wild-type enzyme Campylobacter jejuni
1.1.1.205 9
-
 NAD+ pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant ClpIMPDHDELTAL Clostridium perfringens
1.1.1.205 13
-
 NAD+ pH 8.0, 25°C, recombinant wild-type enzyme Clostridium perfringens
1.1.1.205 13
-
 NAD+ pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant CjIMPDHDELTAS Campylobacter jejuni
1.1.1.205 13
-
 NAD+ pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant VcIMPDHDELTAL Vibrio cholerae serotype O1

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.205 additional information
-
 the inhibitors all exhibit inhibitory potencies with IC50 values of over 0.005 mM with wild-type and truncation mutant Vibrio cholerae serotype O1 additional information
1.1.1.205 0.000006
-
 pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant BaIMPDHDELTAL Bacillus anthracis N-(4-bromophenyl)-N-[1-[3-[1-(hydroxyimino)ethyl]phenyl]-1-methylethyl] urea
1.1.1.205 0.00001
-
 pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant BaIMPDHDELTAL Bacillus anthracis 2-chloro-N-methyl-5-[[[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]amino]carbonyl]aminobenzamide
1.1.1.205 0.000013
-
 pH 8.0, 25°C, recombinant wild-type enzyme Campylobacter jejuni 2-(1-naphthalenyloxy)-N-[(2-(4-pyridinyl)-5-benzoxazolyl)]-(2S)-propanamide
1.1.1.205 0.000015
-
 pH 8.0, 25°C, recombinant wild-type enzyme Clostridium perfringens N-(4-bromophenyl)-N-[(1-methylethenyl)phenyl]ethyl urea
1.1.1.205 0.000019
-
 pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant CjIMPDHDELTAS Campylobacter jejuni 2-(1-naphthalenyloxy)-N-[(2-(4-pyridinyl)-5-benzoxazolyl)]-(2S)-propanamide
1.1.1.205 0.000019
-
 pH 8.0, 25°C, recombinant wild-type enzyme Bacillus anthracis N-(4-bromophenyl)-N-[(1-methylethenyl)phenyl]ethyl urea
1.1.1.205 0.00002
-
 pH 8.0, 25°C, recombinant wild-type enzyme Bacillus anthracis N-(4-bromophenyl)-N-[1-[3-[1-(hydroxyimino)ethyl]phenyl]-1-methylethyl] urea
1.1.1.205 0.000022
-
 pH 8.0, 25°C, recombinant wild-type enzyme Campylobacter jejuni 2-chloro-N-methyl-5-[[[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]amino]carbonyl]aminobenzamide
1.1.1.205 0.000023
-
 pH 8.0, 25°C, recombinant wild-type enzyme Bacillus anthracis 2-(1-naphthalenyloxy)-N-[(2-(4-pyridinyl)-5-benzoxazolyl)]-(2S)-propanamide
1.1.1.205 0.000024
-
 pH 8.0, 25°C, recombinant wild-type enzyme Clostridium perfringens N-(4-bromophenyl)-N-[1-[3-[1-(hydroxyimino)ethyl]phenyl]-1-methylethyl] urea
1.1.1.205 0.000027
-
 pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant BaIMPDHDELTAL Bacillus anthracis 2-(1-naphthalenyloxy)-N-[(2-(4-pyridinyl)-5-benzoxazolyl)]-(2S)-propanamide
1.1.1.205 0.000028
-
 pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant BaIMPDHDELTAS Bacillus anthracis N-(4-bromophenyl)-N-[1-[3-[1-(hydroxyimino)ethyl]phenyl]-1-methylethyl] urea
1.1.1.205 0.000029
-
 pH 8.0, 25°C, recombinant wild-type enzyme Campylobacter jejuni N-(4-bromophenyl)-N-[1-[3-[1-(hydroxyimino)ethyl]phenyl]-1-methylethyl] urea
1.1.1.205 0.000034
-
 pH 8.0, 25°C, recombinant wild-type enzyme Clostridium perfringens 2-chloro-N-methyl-5-[[[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]amino]carbonyl]aminobenzamide
1.1.1.205 0.000036
-
 pH 8.0, 25°C, recombinant wild-type enzyme Campylobacter jejuni N-(4-bromophenyl)-N-[(1-methylethenyl)phenyl]ethyl urea
1.1.1.205 0.000038
-
 pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant BaIMPDHDELTAS Bacillus anthracis 2-(1-naphthalenyloxy)-N-[(2-(4-pyridinyl)-5-benzoxazolyl)]-(2S)-propanamide
1.1.1.205 0.000039
-
 pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant CjIMPDHDELTAS Campylobacter jejuni 2-chloro-N-methyl-5-[[[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]amino]carbonyl]aminobenzamide
1.1.1.205 0.00004
-
 pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant BaIMPDHDELTAS Bacillus anthracis 2-chloro-N-methyl-5-[[[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]amino]carbonyl]aminobenzamide
1.1.1.205 0.000042
-
 pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant CjIMPDHDELTAS Campylobacter jejuni N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
1.1.1.205 0.000043
-
 pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant BaIMPDHDELTAL Bacillus anthracis 4-[(1R)-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4yl]ethoxy]quinoline-1-oxide
1.1.1.205 0.000044
-
 pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant ClpIMPDHDELTAL Clostridium perfringens N-(4-bromophenyl)-N-[(1-methylethenyl)phenyl]ethyl urea
1.1.1.205 0.000046
-
 pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant CjIMPDHDELTAS Campylobacter jejuni N-(4-bromophenyl)-N-[1-[3-[1-(hydroxyimino)ethyl]phenyl]-1-methylethyl] urea
1.1.1.205 0.000047
-
 pH 8.0, 25°C, recombinant wild-type enzyme Bacillus anthracis 2-chloro-N-methyl-5-[[[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]amino]carbonyl]aminobenzamide
1.1.1.205 0.000051
-
 pH 8.0, 25°C, recombinant wild-type enzyme Campylobacter jejuni N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
1.1.1.205 0.000054
-
 pH 8.0, 25°C, recombinant wild-type enzyme Clostridium perfringens 2-(1-naphthalenyloxy)-N-[(2-(4-pyridinyl)-5-benzoxazolyl)]-(2S)-propanamide
1.1.1.205 0.000063
-
 pH 8.0, 25°C, recombinant wild-type enzyme Bacillus anthracis 4-[(1R)-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4yl]ethoxy]quinoline-1-oxide
1.1.1.205 0.000065
-
 pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant BaIMPDHDELTAS Bacillus anthracis N-(4-bromophenyl)-N-[(1-methylethenyl)phenyl]ethyl urea
1.1.1.205 0.000066
-
 pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant ClpIMPDHDELTAL Clostridium perfringens N-(4-bromophenyl)-N-[1-[3-[1-(hydroxyimino)ethyl]phenyl]-1-methylethyl] urea
1.1.1.205 0.000067
-
 pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant CjIMPDHDELTAS Campylobacter jejuni N-(4-bromophenyl)-N-[(1-methylethenyl)phenyl]ethyl urea
1.1.1.205 0.000067
-
 pH 8.0, 25°C, recombinant wild-type enzyme Bacillus anthracis N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
1.1.1.205 0.000072
-
 pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant BaIMPDHDELTAL Bacillus anthracis N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
1.1.1.205 0.000074
-
 pH 8.0, 25°C, recombinant wild-type enzyme Clostridium perfringens 4-[(1R)-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4yl]ethoxy]quinoline-1-oxide
1.1.1.205 0.000092
-
 pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant ClpIMPDHDELTAL Clostridium perfringens 2-chloro-N-methyl-5-[[[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]amino]carbonyl]aminobenzamide
1.1.1.205 0.000095
-
 pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant ClpIMPDHDELTAL Clostridium perfringens 2-(1-naphthalenyloxy)-N-[(2-(4-pyridinyl)-5-benzoxazolyl)]-(2S)-propanamide
1.1.1.205 0.0001
-
 pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant BaIMPDHDELTAS Bacillus anthracis N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
1.1.1.205 0.000107
-
 pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant CjIMPDHDELTAS Campylobacter jejuni 4-[(1R)-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4yl]ethoxy]quinoline-1-oxide
1.1.1.205 0.000137
-
 pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant BaIMPDHDELTAS Bacillus anthracis 4-[(1R)-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4yl]ethoxy]quinoline-1-oxide
1.1.1.205 0.00014
-
 pH 8.0, 25°C, recombinant wild-type enzyme Campylobacter jejuni 4-[(1R)-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4yl]ethoxy]quinoline-1-oxide
1.1.1.205 0.000169
-
 pH 8.0, 25°C, recombinant wild-type enzyme Campylobacter jejuni 3,4-dihydro-3-methyl-4-oxo-N-(6,7,8,9-tetrahydro2-dibenzofuranyl)-1-phthalazineacetamide
1.1.1.205 0.0002
-
 pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant3 CjIMPDHDELTAS Campylobacter jejuni 3,4-dihydro-3-methyl-4-oxo-N-(6,7,8,9-tetrahydro2-dibenzofuranyl)-1-phthalazineacetamide
1.1.1.205 0.000364
-
 pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant ClpIMPDHDELTAL Clostridium perfringens 4-[(1R)-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4yl]ethoxy]quinoline-1-oxide
1.1.1.205 0.00045
-
 pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant ClpIMPDHDELTAL Clostridium perfringens N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
1.1.1.205 0.00057
-
 pH 8.0, 25°C, recombinant wild-type enzyme Clostridium perfringens N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]acetamide
1.1.1.205 0.00067
-
 pH 8.0, 25°C, recombinant wild-type enzyme Bacillus anthracis 3,4-dihydro-3-methyl-4-oxo-N-(6,7,8,9-tetrahydro2-dibenzofuranyl)-1-phthalazineacetamide
1.1.1.205 0.0007
-
 pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant BaIMPDHDELTAL Bacillus anthracis 3,4-dihydro-3-methyl-4-oxo-N-(6,7,8,9-tetrahydro2-dibenzofuranyl)-1-phthalazineacetamide
1.1.1.205 0.0008
-
 pH 8.0, 25°C, recombinant short enzyme CBS-deletion mutant3 BaIMPDHDELTAS Bacillus anthracis 3,4-dihydro-3-methyl-4-oxo-N-(6,7,8,9-tetrahydro2-dibenzofuranyl)-1-phthalazineacetamide
1.1.1.205 0.0017
-
 pH 8.0, 25°C, recombinant wild-type enzyme Clostridium perfringens 3,4-dihydro-3-methyl-4-oxo-N-(6,7,8,9-tetrahydro2-dibenzofuranyl)-1-phthalazineacetamide
1.1.1.205 0.0034
-
 pH 8.0, 25°C, recombinant long enzyme CBS-deletion mutant ClpIMPDHDELTAL Clostridium perfringens 3,4-dihydro-3-methyl-4-oxo-N-(6,7,8,9-tetrahydro2-dibenzofuranyl)-1-phthalazineacetamide

General Information

EC Number General Information Comment Organism
1.1.1.205 malfunction the inhibition of IMPDH leads to the depletion of the guanine nucleotide pool, which blocks proliferation Clostridium perfringens
1.1.1.205 malfunction the inhibition of IMPDH leads to the depletion of the guanine nucleotide pool, which blocks proliferation Vibrio cholerae serotype O1
1.1.1.205 malfunction the inhibition of IMPDH leads to the depletion of the guanine nucleotide pool, which blocks proliferation Campylobacter jejuni
1.1.1.205 malfunction the inhibition of IMPDH leads to the depletion of the guanine nucleotide pool, which blocks proliferation Bacillus anthracis
1.1.1.205 metabolism the enzyme catalyzes the first and rate-limiting step in guanine nucleotide biosynthesis Clostridium perfringens
1.1.1.205 metabolism the enzyme catalyzes the first and rate-limiting step in guanine nucleotide biosynthesis Vibrio cholerae serotype O1
1.1.1.205 metabolism the enzyme catalyzes the first and rate-limiting step in guanine nucleotide biosynthesis Campylobacter jejuni
1.1.1.205 metabolism the enzyme catalyzes the first and rate-limiting step in guanine nucleotide biosynthesis Bacillus anthracis
1.1.1.205 additional information the enzyme has two essential but mutually exclusive conformations, an open conformation that accommodates both the substrate and cofactor during the dehydrogenase step, and a closed conformation where a mobile flap (referred to as the active site flap) moves into the cofactor-binding site for the hydrolysis of E-XMP* Clostridium perfringens
1.1.1.205 additional information the enzyme has two essential but mutually exclusive conformations, an open conformation that accommodates both the substrate and cofactor during the dehydrogenase step, and a closed conformation where a mobile flap (referred to as the active site flap) moves into the cofactor-binding site for the hydrolysis of E-XMP* Vibrio cholerae serotype O1
1.1.1.205 additional information the enzyme has two essential but mutually exclusive conformations, an open conformation that accommodates both the substrate and cofactor during the dehydrogenase step, and a closed conformation where a mobile flap (referred to as the active site flap) moves into the cofactor-binding site for the hydrolysis of E-XMP* Campylobacter jejuni
1.1.1.205 additional information the enzyme has two essential but mutually exclusive conformations, an open conformation that accommodates both the substrate and cofactor during the dehydrogenase step, and a closed conformation where a mobile flap (referred to as the active site flap) moves into the cofactor-binding site for the hydrolysis of E-XMP* Bacillus anthracis