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Literature summary for 1.1.1.205 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
Search for more literature for 1.1.1.205

Application

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

Inhibitors

Inhibitors Comment Organism Structure
NADH mixed inhibition type versus inosine 5'-phosphate and NAD+ Homo sapiens
NADH uncompetitive versus inosine 5'-phosphate and mixed inhibition type versus NAD+ Rattus norvegicus
thiazole-4-carboxamide adenine dinucleotide i.e. TAD, mixed inhibition type versus inosine 5'-phosphate and NAD+ Homo sapiens
thiazole-4-carboxamide adenine dinucleotide i.e. TAD, uncompetitive versus inosine 5'-phosphate and mixed inhibition type versus NAD+ Rattus norvegicus
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
tiazofurin inhibits cell proliferation of hepatoma cells, overview Rattus norvegicus
xanthosine 5'-phosphate competitive versus inosine 5'-phosphate but noncompetitive versus NAD+ Homo sapiens
xanthosine 5'-phosphate competitive versus inosine 5'-phosphate but noncompetitive versus NAD+ Rattus norvegicus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
inosine 5'-phosphate + NAD+ + H2O Homo sapiens rate-limiting step of the de novo guanine nucleotide biosynthesis xanthosine 5'-phosphate + NADH
-
 ?
inosine 5'-phosphate + NAD+ + H2O Rattus norvegicus rate-limiting step of the de novo guanine nucleotide biosynthesis xanthosine 5'-phosphate + NADH
-
 ?
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 ?
-
 ?
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

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

Purification (Commentary)

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

Source Tissue

Source Tissue Comment Organism Textmining
3924A cell hepatoma cell line Rattus norvegicus
-
bone marrow
-
 Homo sapiens
-
cell culture
-
 Homo sapiens
-
erythroleukemia cell
-
 Homo sapiens
-
hepatoma cell
-
 Homo sapiens
-
hepatoma cell
-
 Rattus norvegicus
-
HL-60 cell leukemic cell line Homo sapiens
-
K-562 cell
-
 Homo sapiens
-
myelocytic leukemia cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
inosine 5'-phosphate + NAD+ + H2O rate-limiting step of the de novo guanine nucleotide biosynthesis Homo sapiens xanthosine 5'-phosphate + NADH
-
 ?
inosine 5'-phosphate + NAD+ + H2O rate-limiting step of the de novo guanine nucleotide biosynthesis Rattus norvegicus xanthosine 5'-phosphate + NADH
-
 ?
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 ?
-
 ?
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

Synonyms Comment Organism
IMP DH
-
 Homo sapiens
IMP DH
-
 Rattus norvegicus

Cofactor

Cofactor Comment Organism Structure
NAD+
-
 Homo sapiens
NAD+
-
 Rattus norvegicus

Ki Value [mM]

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