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Literature summary extracted from
- Inosine monophosphate dehydrogenase (IMPDH) as a target in drug discovery (2008), Med. Res. Rev., 28, 219-232.
Application
| EC Number | Application | Comment | Organism |
|---|---|---|---|
| 1.1.1.205 | drug development | differences between the human and Mycobacterium tuberculosis IMPDHs in the region of binding of nucleotide inhibitors on the inosine 5'-phosphate binding site. These and other differences, may be exploited for the design of new inhibitors with selectivity against Mycobacterium tuberculosis IMPDH | Mycobacterium tuberculosis |
| 1.1.1.205 | drug development | type I IMPDH is identified as an antiangiogenic drug target. Inhibition may cause endothelial cell cycle arrest | Homo sapiens |
Crystallization (Commentary)
| EC Number | Crystallization (Comment) | Organism |
|---|---|---|
| 1.1.1.205 | at 2.18 A resolution | Thermotoga maritima |
| 1.1.1.205 | at 2.3 A resolution, in complex with inosine 5'-phosphate and beta-methylene-thiazole-4-carboxyamide-adenine dinucleotide at 2.2 A resolution, in complex with xanthosine 5'-phosphate and NAD+ at 2.15 A resolution, in complex with xanthosine 5'-phosphate and mycophenolic acid at 2.2 A resolution, in complex with RVP and mycophenolic acid at 2.15 A resolution, in complex with 4-carbamoyl-1-beta-D-ribofuranosylimidazolium-5-olate-5'-phosphate at 2.0 A resolution | Tritrichomonas suis |
| 1.1.1.205 | at 2.4 A resolution | Borreliella burgdorferi |
| 1.1.1.205 | in complex with inosine 5'-phosphate and mycophenolic acid at 2.6 A resolution | Cricetulus griseus |
| 1.1.1.205 | in complex with inosine 5'-phosphate at 1.9 A resolution | Streptococcus pyogenes |
| 1.1.1.205 | in complex with xanthosine 5'-phosphate at 2.1 A resolution | Pyrococcus horikoshii OT3 |
| 1.1.1.205 | type I isoform, in complex with 6-chloropurine riboside 5'-monophosphate at 2.5 A resolution | Homo sapiens |
| 1.1.1.205 | type II isoform, in complex with 6-chloropurine riboside 5'-monophosphate and selenazole-4-carboxyamide-adenine dinucleotide at 2.9 A resolution, in complex with ribavirin monophosphate and phosphonic acidmono-[2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-isobenzofuran-5-yl)-ethyl] ester at 2.65 resolution, in complex with with 6-chloropurine riboside 5'-monophosphate and NAD+ at 2.9 A resolution | Homo sapiens |
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 1.1.1.205 | benzamide riboside | inhibitory activity is higher than tiazofurin and lower than selenazofurin; inhibitory activity is higher than tiazofurin and lower than selenazofurin | Homo sapiens |  |
| 1.1.1.205 | beta-methylene-thiazole-4-carboxyamide-adenine dinucleotide | - |
Tritrichomonas suis | |
| 1.1.1.205 | BMS-337197 | is a potent IMPDH inhibitor, shows in vivo activity for inhibition of antibody production in mice | Mus musculus | |
| 1.1.1.205 | BMS-337197 | is a potent IMPDH inhibitor, shows in vivo activity for inhibition of antibody production in the adjuvant-induced arthritis model in rats | Rattus norvegicus | |
| 1.1.1.205 | Mycophenolic acid | - |
Cricetulus griseus | |
| 1.1.1.205 | Mycophenolic acid | - |
Escherichia coli | |
| 1.1.1.205 | Mycophenolic acid | is a uncompetitive inhibitor of IMPDH with respect to both inosine 5'-phosphate and NAD+, inhibits IMPDH by trapping the covalent intermediate. It it is easily converted to mycophenolic acid-7-O-glucuronide, which limits the inhibitory efficacy and higher doses are therefore needed in order to maintain appropriate therapeutic levels; is a uncompetitive inhibitor of IMPDH with respect to both inosine 5'-phosphate and NAD+, inhibits IMPDH by trapping the covalent intermediate. It it is easily converted to mycophenolic acid-7-O-glucuronide, which limits the inhibitory efficacy and higher doses are therefore needed in order to maintain appropriate therapeutic levels | Homo sapiens | |
| 1.1.1.205 | Mycophenolic acid | - |
Leishmania donovani | |
| 1.1.1.205 | Mycophenolic acid | - |
Tritrichomonas suis | |
| 1.1.1.205 | NAD+ | - |
Tritrichomonas suis | |
| 1.1.1.205 | ribavirin monophosphate | - |
Homo sapiens | |
| 1.1.1.205 | ribavirin monophosphate | - |
Mycobacterium tuberculosis | |
| 1.1.1.205 | Selenazofurin | - |
Homo sapiens | |
| 1.1.1.205 | selenazole-4-carboxyamide-adenine dinucleotide | - |
Homo sapiens | |
| 1.1.1.205 | tiazofurin | - |
Homo sapiens | |
| 1.1.1.205 | VX-148 | - |
Homo sapiens | |
| 1.1.1.205 | VX-497 | - |
Homo sapiens | |
Molecular Weight [Da]
| EC Number | Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
|---|---|---|---|---|
| 1.1.1.205 | 56000 | - |
4 * 56000 | Homo sapiens |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 1.1.1.205 | Borreliella burgdorferi | - |
- |
- |
| 1.1.1.205 | Cricetulus griseus | - |
chinese hamster | - |
| 1.1.1.205 | Escherichia coli | - |
- |
- |
| 1.1.1.205 | Homo sapiens | P12268 | - |
- |
| 1.1.1.205 | Homo sapiens | P20839 | - |
- |
| 1.1.1.205 | Leishmania donovani | - |
- |
- |
| 1.1.1.205 | Mus musculus | - |
- |
- |
| 1.1.1.205 | Mycobacterium tuberculosis | - |
strains CDC1551 and H37Rv | - |
| 1.1.1.205 | Pyrococcus horikoshii OT3 | - |
- |
- |
| 1.1.1.205 | Rattus norvegicus | - |
- |
- |
| 1.1.1.205 | Streptococcus pyogenes | - |
- |
- |
| 1.1.1.205 | Thermotoga maritima | - |
- |
- |
| 1.1.1.205 | Tritrichomonas suis | - |
- |
- |
Source Tissue
| EC Number | Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|---|
| 1.1.1.205 | carcinoma cell | - |
Homo sapiens | - |
| 1.1.1.205 | carcinoma cell | type II isoform predominates | Homo sapiens | - |
| 1.1.1.205 | K-562 cell | - |
Homo sapiens | - |
| 1.1.1.205 | leukocyte | - |
Homo sapiens | - |
| 1.1.1.205 | leukocyte | type I isoform is prevalent | Homo sapiens | - |
| 1.1.1.205 | lymphocyte | - |
Homo sapiens | - |
| 1.1.1.205 | lymphocyte | type I isoform is prevalent | Homo sapiens | - |
| 1.1.1.205 | additional information | type II isoform predominates in proliferating cells and is upregulated in neoplastic cells | Homo sapiens | - |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 1.1.1.205 | inosine 5'-phosphate + NAD+ + H2O | - |
Homo sapiens | xanthosine 5'-phosphate + NADH | - |
? | |
| 1.1.1.205 | inosine 5'-phosphate + NAD+ + H2O | - |
Cricetulus griseus | xanthosine 5'-phosphate + NADH + H+ | - |
? | |
| 1.1.1.205 | inosine 5'-phosphate + NAD+ + H2O | - |
Mus musculus | xanthosine 5'-phosphate + NADH + H+ | - |
? | |
| 1.1.1.205 | inosine 5'-phosphate + NAD+ + H2O | - |
Escherichia coli | xanthosine 5'-phosphate + NADH + H+ | - |
? | |
| 1.1.1.205 | inosine 5'-phosphate + NAD+ + H2O | - |
Rattus norvegicus | xanthosine 5'-phosphate + NADH + H+ | - |
? | |
| 1.1.1.205 | inosine 5'-phosphate + NAD+ + H2O | - |
Streptococcus pyogenes | xanthosine 5'-phosphate + NADH + H+ | - |
? | |
| 1.1.1.205 | inosine 5'-phosphate + NAD+ + H2O | - |
Mycobacterium tuberculosis | xanthosine 5'-phosphate + NADH + H+ | - |
? | |
| 1.1.1.205 | inosine 5'-phosphate + NAD+ + H2O | - |
Leishmania donovani | xanthosine 5'-phosphate + NADH + H+ | - |
? | |
| 1.1.1.205 | inosine 5'-phosphate + NAD+ + H2O | - |
Thermotoga maritima | xanthosine 5'-phosphate + NADH + H+ | - |
? | |
| 1.1.1.205 | inosine 5'-phosphate + NAD+ + H2O | - |
Tritrichomonas suis | xanthosine 5'-phosphate + NADH + H+ | - |
? | |
| 1.1.1.205 | inosine 5'-phosphate + NAD+ + H2O | - |
Borreliella burgdorferi | xanthosine 5'-phosphate + NADH + H+ | - |
? | |
| 1.1.1.205 | inosine 5'-phosphate + NAD+ + H2O | - |
Pyrococcus horikoshii OT3 | xanthosine 5'-phosphate + NADH + H+ | - |
? | |
Subunits
| EC Number | Subunits | Comment | Organism |
|---|---|---|---|
| 1.1.1.205 | tetramer | 4 * 56000 | Homo sapiens |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 1.1.1.205 | IMPDH | - |
Cricetulus griseus |
| 1.1.1.205 | IMPDH | - |
Mus musculus |
| 1.1.1.205 | IMPDH | - |
Escherichia coli |
| 1.1.1.205 | IMPDH | - |
Rattus norvegicus |
| 1.1.1.205 | IMPDH | - |
Streptococcus pyogenes |
| 1.1.1.205 | IMPDH | - |
Mycobacterium tuberculosis |
| 1.1.1.205 | IMPDH | - |
Leishmania donovani |
| 1.1.1.205 | IMPDH | - |
Thermotoga maritima |
| 1.1.1.205 | IMPDH | - |
Tritrichomonas suis |
| 1.1.1.205 | IMPDH | - |
Borreliella burgdorferi |
| 1.1.1.205 | IMPDH | - |
Pyrococcus horikoshii OT3 |
| 1.1.1.205 | IMPDH | - |
Homo sapiens |
| 1.1.1.205 | inosine monophosphate dehydrogenase | - |
Cricetulus griseus |
| 1.1.1.205 | inosine monophosphate dehydrogenase | - |
Mus musculus |
| 1.1.1.205 | inosine monophosphate dehydrogenase | - |
Escherichia coli |
| 1.1.1.205 | inosine monophosphate dehydrogenase | - |
Rattus norvegicus |
| 1.1.1.205 | inosine monophosphate dehydrogenase | - |
Streptococcus pyogenes |
| 1.1.1.205 | inosine monophosphate dehydrogenase | - |
Mycobacterium tuberculosis |
| 1.1.1.205 | inosine monophosphate dehydrogenase | - |
Leishmania donovani |
| 1.1.1.205 | inosine monophosphate dehydrogenase | - |
Thermotoga maritima |
| 1.1.1.205 | inosine monophosphate dehydrogenase | - |
Tritrichomonas suis |
| 1.1.1.205 | inosine monophosphate dehydrogenase | - |
Borreliella burgdorferi |
| 1.1.1.205 | inosine monophosphate dehydrogenase | - |
Pyrococcus horikoshii OT3 |
| 1.1.1.205 | inosine monophosphate dehydrogenase | - |
Homo sapiens |
Cofactor
| EC Number | Cofactor | Comment | Organism | Structure |
|---|---|---|---|---|
| 1.1.1.205 | NAD+ | - |
Mycobacterium tuberculosis | |
| 1.1.1.205 | NAD+ | dependent on | Cricetulus griseus | |
| 1.1.1.205 | NAD+ | dependent on | Mus musculus | |
| 1.1.1.205 | NAD+ | dependent on | Escherichia coli | |
| 1.1.1.205 | NAD+ | dependent on | Rattus norvegicus | |
| 1.1.1.205 | NAD+ | dependent on | Streptococcus pyogenes | |
| 1.1.1.205 | NAD+ | dependent on | Leishmania donovani | |
| 1.1.1.205 | NAD+ | dependent on | Thermotoga maritima | |
| 1.1.1.205 | NAD+ | dependent on | Tritrichomonas suis | |
| 1.1.1.205 | NAD+ | dependent on | Borreliella burgdorferi | |
| 1.1.1.205 | NAD+ | dependent on | Pyrococcus horikoshii OT3 | |
| 1.1.1.205 | NAD+ | dependent on | Homo sapiens | |
Ki Value [mM]
| EC Number | Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 1.1.1.205 | 0.0000002 | - |
Mycophenolic acid | - |
Leishmania donovani | |
| 1.1.1.205 | 0.000007 | - |
Mycophenolic acid | against type II isoform | Homo sapiens | |
| 1.1.1.205 | 0.000007 | - |
VX-497 | type I isoform | Homo sapiens | |
| 1.1.1.205 | 0.000009 | - |
Mycophenolic acid | - |
Tritrichomonas suis | |
| 1.1.1.205 | 0.00001 | - |
VX-497 | against type II isoform | Homo sapiens | |
| 1.1.1.205 | 0.00002 | - |
Mycophenolic acid | - |
Escherichia coli | |
| 1.1.1.205 | 0.00002 | - |
Mycophenolic acid | against IMPDH in general | Homo sapiens | |
| 1.1.1.205 | 0.000033 | - |
Mycophenolic acid | type I isoform | Homo sapiens | |
General Information
| EC Number | General Information | Comment | Organism |
|---|---|---|---|
| 1.1.1.205 | physiological function | is a key enzyme in the biosynthesis of purine nucleotides | Cricetulus griseus |
| 1.1.1.205 | physiological function | is a key enzyme in the biosynthesis of purine nucleotides | Escherichia coli |
| 1.1.1.205 | physiological function | is a key enzyme in the biosynthesis of purine nucleotides | Rattus norvegicus |
| 1.1.1.205 | physiological function | is a key enzyme in the biosynthesis of purine nucleotides | Streptococcus pyogenes |
| 1.1.1.205 | physiological function | is a key enzyme in the biosynthesis of purine nucleotides | Leishmania donovani |
| 1.1.1.205 | physiological function | is a key enzyme in the biosynthesis of purine nucleotides | Thermotoga maritima |
| 1.1.1.205 | physiological function | is a key enzyme in the biosynthesis of purine nucleotides | Tritrichomonas suis |
| 1.1.1.205 | physiological function | is a key enzyme in the biosynthesis of purine nucleotides | Borreliella burgdorferi |
| 1.1.1.205 | physiological function | is a key enzyme in the biosynthesis of purine nucleotides | Pyrococcus horikoshii OT3 |
| 1.1.1.205 | physiological function | is a key enzyme in the biosynthesis of purine nucleotides | Homo sapiens |
| 1.1.1.205 | physiological function | is a key enzyme in the biosynthesis of purine nucleotides. Loss of both alleles of the type 2 gene results in very early embryonic lethality. Type I enzymatic activity appears not to be essential for normal mouse development or fertility | Mus musculus |
| 1.1.1.205 | physiological function | is a key enzyme in the biosynthesis of purine nucleotides. Mutations in the type I gene cause the RP10 form of autosomal dominant retinitis pigmentosa | Homo sapiens |
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