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Literature summary extracted from

  • Franchetti, P.; Cappellacci, L.; Pasqualini, M.; Petrelli, R.; Jayaprakasan, V.; Jayaram, H.N.; Boyd, D.B.; Jain, M.D.; Grifantini, M.
    Synthesis, conformational analysis, and biological activity of new analogues of thiazole-4-carboxamide adenine dinucleotide (TAD) as IMP dehydrogenase inhibitors (2005), Bioorg. Med. Chem., 13, 2045-2053.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.1.1.205 expression of isoyzmes IMPDH I and IMPDH II in Escherichia coli strain BL21(DE3) Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.205 2'-methylthiazole-4-carboxamide adenine dinucleotide noncompetitive inhibition, less cytotoxic against K562 tumor cells Homo sapiens
1.1.1.205 3'-methylthiazole-4-carboxamide adenine dinucleotide noncompetitive inhibition, less cytotoxic against K562 tumor cells Homo sapiens
1.1.1.205 beta-methylene-TAD noncompetitive inhibition Homo sapiens
1.1.1.205 thiazole-4-carboxamide adenine dinucleotide i.e. TAD, synthesis, noncompetitive inhibition, conformational analysis, and biological activity of inhibitor analogues, overview, TAD binds to the NAD+ binding site with out isozyme specificity, mechanism and molecular modeling using the enzyme crystal structure, overview, cytotoxic against K562 tumor cells Homo sapiens
1.1.1.205 tiazofurin noncompetitive inhibition, cytotoxic against K562 tumor cells Homo sapiens

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
-
 ir

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.205 Homo sapiens
-
 type I and type II isozymes
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.1.1.205 recombinant isoyzmes IMPDH I and IMPDH II from Escherichia coli strain BL21(DE3) by two steps of ion exchange chromatography 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
-
 ir
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
-
 ir

Subunits

EC Number Subunits Comment Organism
1.1.1.205 tetramer
-
 Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
1.1.1.205 IMPDH II
-
 Homo sapiens
1.1.1.205 inosine 5'-monophosphate dehydrogenase
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
1.1.1.205 37
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.1.1.205 8
-
 assay at Homo sapiens

Cofactor

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

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.1.1.205 additional information
-
 additional information inhibition patterns, isozymes I and II Homo sapiens
1.1.1.205 0.00019
-
 thiazole-4-carboxamide adenine dinucleotide isozyme IMPDH I Homo sapiens
1.1.1.205 0.00024
-
 thiazole-4-carboxamide adenine dinucleotide isozyme IMPDH II Homo sapiens
1.1.1.205 0.00052
-
 3'-methylthiazole-4-carboxamide adenine dinucleotide isozyme IMPDH I Homo sapiens
1.1.1.205 0.00066
-
 3'-methylthiazole-4-carboxamide adenine dinucleotide isozyme IMPDH II Homo sapiens
1.1.1.205 0.0011
-
 2'-methylthiazole-4-carboxamide adenine dinucleotide isozyme IMPDH I Homo sapiens
1.1.1.205 0.0014
-
 2'-methylthiazole-4-carboxamide adenine dinucleotide isozyme IMPDH II Homo sapiens