Literature summary for 1.1.1.205 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.

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Cloned(Commentary)

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

Inhibitors

Inhibitors	Comment	Organism	Structure
2'-methylthiazole-4-carboxamide adenine dinucleotide	noncompetitive inhibition, less cytotoxic against K562 tumor cells	Homo sapiens
3'-methylthiazole-4-carboxamide adenine dinucleotide	noncompetitive inhibition, less cytotoxic against K562 tumor cells	Homo sapiens
beta-methylene-TAD	noncompetitive inhibition	Homo sapiens
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
tiazofurin	noncompetitive inhibition, cytotoxic against K562 tumor cells	Homo sapiens

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	-	ir

Organism

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

Purification (Commentary)

Purification (Comment)	Organism
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)

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

Subunits

Subunits	Comment	Organism
tetramer	-	Homo sapiens

Synonyms

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

Temperature Optimum [°C]

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

pH Optimum

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

Cofactor

Cofactor	Comment	Organism	Structure
NAD+	-	Homo sapiens

Ki Value [mM]

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

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Release 2023.1 (January 2023)