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Literature summary extracted from

  • Weber, G.; Yamaji, Y.; Olah, E.; Natsumeda, Y.; Jayaram, H.N.; Lapis, E.; Zhen, W.; Prajda, N.; Hoffman, R.; Tricot, G.J.
    Clinical and molecular impact of inhibition of IMP dehydrogenase activity by tiazofurin (1989), Adv. Enzyme Regul., 28, 335-356.
    View publication on PubMed

Application

EC Number Application Comment Organism
1.1.1.205 drug development the enzyme is a target in enzyme-pattern-targeted chemotherapy in acuet leukemia, AML, treatment Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.205 NADH mixed inhibition type versus inosine 5'-phosphate and NAD+ Homo sapiens
1.1.1.205 NADH uncompetitive versus inosine 5'-phosphate and mixed inhibition type versus NAD+ Rattus norvegicus
1.1.1.205 thiazole-4-carboxamide adenine dinucleotide i.e. TAD, mixed inhibition type versus inosine 5'-phosphate and NAD+ Homo sapiens
1.1.1.205 thiazole-4-carboxamide adenine dinucleotide i.e. TAD, uncompetitive versus inosine 5'-phosphate and mixed inhibition type versus NAD+ Rattus norvegicus
1.1.1.205 tiazofurin i.e. 2-beta-D-ribofuranosyl-thiazole-4-carboxamide, overview: clinical and molecular impact of inhibition; the drug is tested in clinical use to treat acute myelocytic leukemia, AML, detailed overview, tiazofurin treatment may result in induced differentiation of leukemic leukocytes in patients, incubation of K-562 cells with tiazofurin produces inhibition of IMP DH and decreases GTP concentration, these biochemical alterations are followed by a decrease in the expression of as proto-oncogene which is followed by induced differentiation of these cells, biochemical mechanism, overview Homo sapiens
1.1.1.205 tiazofurin inhibits cell proliferation of hepatoma cells, overview Rattus norvegicus
1.1.1.205 xanthosine 5'-phosphate competitive versus inosine 5'-phosphate but noncompetitive versus NAD+ Homo sapiens
1.1.1.205 xanthosine 5'-phosphate competitive versus inosine 5'-phosphate but noncompetitive versus NAD+ Rattus norvegicus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.1.1.205 inosine 5'-phosphate + NAD+ + H2O Homo sapiens rate-limiting step of the de novo guanine nucleotide biosynthesis xanthosine 5'-phosphate + NADH
-
 ?
1.1.1.205 inosine 5'-phosphate + NAD+ + H2O Rattus norvegicus rate-limiting step of the de novo guanine nucleotide biosynthesis xanthosine 5'-phosphate + NADH
-
 ?
1.1.1.205 additional information Homo sapiens increased activities of IMP DH and GMP synthase and in the elevated concentrations of guanylates in hepatomas and other tumor cells ?
-
 ?
1.1.1.205 additional information Rattus norvegicus increased activities of IMP DH and GMP synthase and in the elevated concentrations of guanylates in hepatomas and other tumor cells ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.205 Homo sapiens
-
-
-
1.1.1.205 Rattus norvegicus
-
-
-
1.1.1.205 Rattus norvegicus
-
 hepatoma 3924A
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.1.1.205 native enzyme from hepatoma 3924A cells to homogeneity Rattus norvegicus

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.1.1.205 3924A cell hepatoma cell line Rattus norvegicus
-
1.1.1.205 bone marrow
-
 Homo sapiens
-
1.1.1.205 cell culture
-
 Homo sapiens
-
1.1.1.205 erythroleukemia cell
-
 Homo sapiens
-
1.1.1.205 hepatoma cell
-
 Homo sapiens
-
1.1.1.205 hepatoma cell
-
 Rattus norvegicus
-
1.1.1.205 HL-60 cell leukemic cell line Homo sapiens
-
1.1.1.205 K-562 cell
-
 Homo sapiens
-
1.1.1.205 myelocytic leukemia cell
-
 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 rate-limiting step of the de novo guanine nucleotide biosynthesis Homo sapiens xanthosine 5'-phosphate + NADH
-
 ?
1.1.1.205 inosine 5'-phosphate + NAD+ + H2O rate-limiting step of the de novo guanine nucleotide biosynthesis Rattus norvegicus xanthosine 5'-phosphate + NADH
-
 ?
1.1.1.205 additional information increased activities of IMP DH and GMP synthase and in the elevated concentrations of guanylates in hepatomas and other tumor cells Homo sapiens ?
-
 ?
1.1.1.205 additional information increased activities of IMP DH and GMP synthase and in the elevated concentrations of guanylates in hepatomas and other tumor cells Rattus norvegicus ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.1.1.205 IMP DH
-
 Homo sapiens
1.1.1.205 IMP DH
-
 Rattus norvegicus

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.205 NAD+
-
 Homo sapiens
1.1.1.205 NAD+
-
 Rattus norvegicus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.1.1.205 additional information
-
 additional information
-
 Homo sapiens
1.1.1.205 additional information
-
 additional information various inhibitors Rattus norvegicus
1.1.1.205 additional information
-
 additional information inhibition kinetics Homo sapiens
1.1.1.205 additional information
-
 additional information inhibition kinetics Rattus norvegicus
1.1.1.205 0.00029
-
 thiazole-4-carboxamide adenine dinucleotide versus inosine 5'-phosphate Homo sapiens
1.1.1.205 0.00031
-
 thiazole-4-carboxamide adenine dinucleotide versus inosine 5'-phosphate Rattus norvegicus
1.1.1.205 0.00073
-
 thiazole-4-carboxamide adenine dinucleotide versus NAD+ Rattus norvegicus
1.1.1.205 0.00074
-
 thiazole-4-carboxamide adenine dinucleotide versus NAD+ Homo sapiens
1.1.1.205 0.118
-
 xanthosine 5'-phosphate versus inosine 5'-phosphate Homo sapiens
1.1.1.205 0.136
-
 xanthosine 5'-phosphate versus inosine 5'-phosphate Rattus norvegicus
1.1.1.205 0.21
-
 NADH versus inosine 5'-phosphate Rattus norvegicus
1.1.1.205 0.23
-
 NADH versus inosine 5'-phosphate Homo sapiens
1.1.1.205 0.28
-
 xanthosine 5'-phosphate versus NAD+ Homo sapiens
1.1.1.205 0.287
-
 NADH versus NAD+ Rattus norvegicus
1.1.1.205 0.32
-
 xanthosine 5'-phosphate versus NAD+ Rattus norvegicus
1.1.1.205 0.38
-
 NADH versus NAD+ Homo sapiens