1.1.1.205: IMP dehydrogenase

This is an abbreviated version!
For detailed information about IMP dehydrogenase, go to the full flat file.

Reaction

Synonyms

A1S_3321, BTH_I2056, class I IMPDH, class II IMPDH, dehydrogenase, inosinate, DR63_268, EC 1.2.1.14, GBAA_0008, guaB, guaB2, IMD2, IMD3, IMD4, IMP dehydrogenase, IMP DH, IMP oxidoreductase, IMP-DH, IMP:NAD oxidoreductase, IMP:NAD+ oxidoreductase, IMPD, IMPDH, IMPDH II, IMPDH-1, IMPDH-B, IMPDH-S, IMPDH1, IMPDH2, IMPDHA, IMPDHab, IMPDHba, IMPDHbt, IMPDHI, IMPDHII, IMPDHkp, IMPDHlpp, IMPDHnm, IMPDHpa, inosinate dehydrogenase, inosine 5' monophosphate dehydrogenase, inosine 5'-monophosphate dehydrogenase, inosine 5'-monophosphate dehydrogenase 2, inosine 5'-phosphate dehydrogenase, inosine 5-monophosphate dehydrogenase, inosine 5-monophosphate dehydrogenase 2, inosine 5-monophosphate dehydrogenase type I, inosine 5� -monophosphate dehydrogenase, inosine 5�-monophosphate dehydrogenase 2, inosine monophosphate dehydrogenase, inosine monophosphate dehydrogenase-1, inosine monophosphate dehydrogenase-2, inosine monophosphate oxidoreductase, inosine-5'-monophosphate dehydrogenase, inosine-5'-phosphate dehydrogenase, inosine-5-monophosphate dehydrogenase, inosinic acid 5�-monophosphate dehydrogenase, inosinic acid dehydrogenase, lpg1723, mpaF, NMC1103, Raspberry protein, Rv3411c, SOI12, Superoxide-inducible protein 12, type 1 inosine monophosphate, type 2 inosine monophosphate dehydrogenase

ECTree

     1 Oxidoreductases

         1.1 Acting on the CH-OH group of donors

             1.1.1 With NAD⁺ or NADP⁺ as acceptor

                1.1.1.205 IMP dehydrogenase

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Results	in table
37	Activating Compound
43951	AA Sequence
38	Application
1	CAS Registry Number
83	Cloned(Commentary)
197	Cofactor
44	Crystallization (Commentary)
1367	Disease/ Diagnostics
5	Expression
126	General Information
8	General Stability
294	IC50 Value
1189	Inhibitors
5	kcat/KM [mM/s]
366	Ki Value [mM]
230	KM Value [mM]
13	Localization
72	Metals/Ions
75	Molecular Weight [Da]
133	Natural Substrates/ Products (Substrates)
2	Organic Solvent Stability
726	Organism
9	Pathway
561	PDB ID
57	pH Optimum
11	pH Range
105	Protein Variants
87	Purification (Commentary)
29	Reaction
3	Reaction Type
312	Reference
2	Renatured (Commentary)
132	Source Tissue
39	Specific Activity [micromol/min/mg]
18	Storage Stability
292	Substrates and Products (Substrate)
80	Subunits
431	Synonyms
1	Systematic Name
41	Temperature Optimum [°C]
1	Temperature Range [°C]
4	Temperature Stability [°C]
93	Turnover Number [1/s]

Application

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Application on EC 1.1.1.205 - IMP dehydrogenase

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APPLICATION

ORGANISM

UNIPROT

COMMENTARY

LITERATURE

analysis

Homo sapiens

-

real-time reverse-transcription PCR assay for mRNA quantification of isoforms IMPDH1 and IMPDH2 in blood samples and cultured cells. Limits of detection and quantification are 10 and 1000 copies of cDNA per reaction, respectively

686145

diagnostics

Homo sapiens

P12268, P20839

IMPDH activity is measured in adults without thiopurine treatment as well as in adult and paediatric patients treated with thiopurines. A wide interindividual variability in IMPDH activity in erythrocytes is observed. No difference in IMPDH activity is found between untreated subjects and adult and paediatric patients on thiopurine therapy. The method described is useful in the determination of IMPDH phenotype from patients on thiopurine therapy and in the investigation of the potential relationship between IMPDH activity in erythrocytes and the occurrence of adverse events and drug response variability

740801

drug development

19 entries

medicine

16 entries

pharmacology

Homo sapiens

-

the enzyme is a potential target as modulators in MTX chemotherapy of resistant cells, overview

670128

drug development

Tritrichomonas suis

-

the enzyme is a potential therapeutic target, and the NAD+ site may be an exploitable target for the design of antimicrobial drugs

667573

drug development

Homo sapiens

-

the enzyme is a target for drug development in treatment of structural schizophrenia

668351

drug development

Homo sapiens

-

the enzyme is a target for therapeutic drugs

669807

drug development

Homo sapiens

-

the enzyme is a target in enzyme-pattern-targeted chemotherapy in acuet leukemia, AML, treatment

347916

drug development

Toxoplasma gondii

Q4VRV8

the enzyme is a target in parasite treatment and elimination

667219

drug development

Homo sapiens

-

the IMPDH-1 is an antiangiogenic drug target

669800

drug development

Cryptosporidium parvum

-

1,2,3-triazole IMPDH inhibitors provide new tools for elucidating the role of IMPDH in Cryptosporidium parvum and may serve as potential therapeutics for treating cryptosporidiosis

705042

drug development

Homo sapiens

-

at therapeutic concentrations in organ transplant patients, the effect of mycophenolic acid-acyl-glucuronide on IMPDHII activity is minimal compared to mycophenolic acid, and the quantification of mycophenolic acid metabolites for mycophenolate therapeutic drug monitoring and dose adjustment will be of no benefit

703271

drug development

Mycobacterium tuberculosis

-

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

705494

drug development

Homo sapiens

P12268, P20839

IMPDH2 is the major target for cancer chemotherapy

703193

drug development

Homo sapiens

-

Roche total mycophenolic acid assay (a new inosine monophosphate dehydrogenase inhibition assay) is a promising alternative for mycophenolic acid quantification where chromatographic methods are not available

706815

drug development

Homo sapiens

P12268, P20839

type I IMPDH is identified as an antiangiogenic drug target. Inhibition may cause endothelial cell cycle arrest

705494

drug development

Mycobacterium tuberculosis

P9WKI7

IMPDH from Mycobacterium tuberculosis (MtIMPDH) is a potential molecular target to inhibitor development

741400

drug development

Mycobacterium tuberculosis

P9WKI7

inosine 5'-monophosphate dehydrogenase 2 (IMPDH2) from Mycobacterium tuberculosis is an attractive drug target

741245

drug development

Cryptosporidium parvum

Q8T6T2

the enzyme IMPDH is a promising target for the treatment of Cryptosporidium infections

739820

drug development

Homo sapiens

P12268

the inhibition of IMPDH (leading to reduced cellular levels of guanine nucleotides) is an important strategy for antiproliferative, antiviral and antiparasitic effects. It is also a useful strategy for producing immunosuppression as IMPDH-dependent de novo synthesis of guanine nucleotides is responsible for maintaining the growth and differentiation of human B and T lymphocytes

740808

drug development

Mycobacterium tuberculosis H37Rv

-

inosine 5'-monophosphate dehydrogenase 2 (IMPDH2) from Mycobacterium tuberculosis is an attractive drug target

-

drug development

Mycobacterium tuberculosis H37Rv

-

IMPDH from Mycobacterium tuberculosis (MtIMPDH) is a potential molecular target to inhibitor development

-

drug development

Cryptosporidium parvum Iowa II

-

the enzyme IMPDH is a promising target for the treatment of Cryptosporidium infections

-

medicine

Homo sapiens

-

the enzyme is a major therapeutic target

669476

medicine

Homo sapiens

-

the enzyme is a target for immunosuppression therapy suing mycophenolic acid, prodrug is mycophenolate mofetil

670881

medicine

Homo sapiens

-

changes in expression of IMPDH1 and IMPDH2 in patient samples after initiation of an immunosuppressive regimen that includes calcineurin inhibitors, mycophenolate mofetil, and stroids

686145

medicine

Homo sapiens

-

in patients with kidney transplantation, type I IMPDH activity and gene expression increases during the first three months following transplantation and reaches its maximal level during acute rejection episodes, whereas type II mRNA is stable. Patients with a prolonged mycophenolate mofetil treatment exhibit an increase in the induction potency of both IMPDH activity and gene expression. Measurement of IMPDH mRNAs may provide reliable information to predict acute rejection

686191

medicine

Homo sapiens

-

in renal transplant patients, transplantation and initiation of immunosuppressive therapy is associated with increased isoform IMPDH1 and decreased IMPDH2 expression. In CD4+ cells, however, IMPDH2 expression increases. Two weeks posttransplant, mycophenolic acid-treated patients display elevated IMPDH1 and IMPDH2 expression in reticulocyte. Patients with acute rejection during follow-up demonstrate higher IMPDH2 expression in Cd4+ cells pretransplant than nonrejecting patients

690165

medicine

Homo sapiens

-

in stable kidney transplant recipients, inosine 5'-phosphate dehydrogenase activity is 17.5 versus 46.6 nmol XMP/h/microgramm protein in diabetic and nondiabetic patients, respectively. Activity in diabetic patients is significantly lower irrespective of concomitant therapy with cyclosporine or tacrolimus and independent of the bound or unbound mycophenolic acid

690117

medicine

Homo sapiens

-

study on inosine 5'-phosphate activity in thiopurine-treated patients with inflammatory bowel disease. Negative correlation between inosine 5'-phosphate dehydrogenase activity and dose-normalized 6-methylthioinosine concentrations, no evident correlation to 6-thioguanine nucleotide or the 6-methylthioinosine/6-thioguanine nucleotide ratio

685852

medicine

Homo sapiens

-

a poorer response to mycophenolic acid therapy in some individuals may be due to the presence of the rs11706052 polymorphism

706090

medicine

Homo sapiens

-

IMPDH activity in erythrocytes may be useful indicator of short-term immunosuppression and long-term exposure of the immunosuppressant mycophenolic acid

703272

medicine

Mus musculus

-

inhibition of IMPDH may represent a novel strategy to reduce adipose tissue mass

702061

medicine

Homo sapiens

-

modified method for the measurement of IMPDH activity, that is less labor-intensive, more robust in general, and capable of yielding a better reproducibility, which can be used reliably in multicenter trials and in longitudinal studies to evaluate the additional value of any pharmacodynamic monitoring among a diversity of patients treated with mycophenolic acid

706817

medicine

Homo sapiens

-

study on a target range for inosine 5'-monophosphate dehydrogenase activity in maintenance therapy with tacrolimus, on patients with renal transplants and healthy volunteers. Inosine 5'-monophosphate dehydrogenase activity in cell lysates can be reliably determined indirectly by measuring xanthosine 5'-monophophate in cell lysates supplemented with IMP and beta-nicotine adenine dinucleotide using an HPLC method. Cell lysates show a 5-6 nmol /l IC50 mycophenolic acid concentration. Tacrolimus, cyclosporine and prednisolone do not affect IMPDH activity. The peak mycophenolic acid concentration is achieved at 1 h after dosing. IMPDH activity decreases to 75% and 67% at 1 and 2 h after dosing respectively

712578

medicine

Clostridium perfringens

-

MPDH inhibitors are used as immunosuppressive, antiviral, and anticancer agents

740742

medicine

Vibrio cholerae serotype O1

-

MPDH inhibitors are used as immunosuppressive, antiviral, and anticancer agents

740742

medicine

Campylobacter jejuni

-

MPDH inhibitors are used as immunosuppressive, antiviral, and anticancer agents

740742

medicine

Bacillus anthracis

-

MPDH inhibitors are used as immunosuppressive, antiviral, and anticancer agents

740742