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analysis
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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
diagnostics
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
pharmacology
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the enzyme is a potential target as modulators in MTX chemotherapy of resistant cells, overview
drug development
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the enzyme is a potential therapeutic target, and the NAD+ site may be an exploitable target for the design of antimicrobial drugs
drug development
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the enzyme is a target for drug development in treatment of structural schizophrenia
drug development
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the enzyme is a target for therapeutic drugs
drug development
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the enzyme is a target in enzyme-pattern-targeted chemotherapy in acuet leukemia, AML, treatment
drug development
the enzyme is a target in parasite treatment and elimination
drug development
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the IMPDH-1 is an antiangiogenic drug target
drug development
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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
drug development
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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
drug development
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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
drug development
IMPDH2 is the major target for cancer chemotherapy
drug development
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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
drug development
type I IMPDH is identified as an antiangiogenic drug target. Inhibition may cause endothelial cell cycle arrest
drug development
IMPDH from Mycobacterium tuberculosis (MtIMPDH) is a potential molecular target to inhibitor development
drug development
inosine 5'-monophosphate dehydrogenase 2 (IMPDH2) from Mycobacterium tuberculosis is an attractive drug target
drug development
the enzyme IMPDH is a promising target for the treatment of Cryptosporidium infections
drug development
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
drug development
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inosine 5'-monophosphate dehydrogenase 2 (IMPDH2) from Mycobacterium tuberculosis is an attractive drug target
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drug development
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IMPDH from Mycobacterium tuberculosis (MtIMPDH) is a potential molecular target to inhibitor development
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drug development
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the enzyme IMPDH is a promising target for the treatment of Cryptosporidium infections
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medicine
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the enzyme is a major therapeutic target
medicine
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the enzyme is a target for immunosuppression therapy suing mycophenolic acid, prodrug is mycophenolate mofetil
medicine
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changes in expression of IMPDH1 and IMPDH2 in patient samples after initiation of an immunosuppressive regimen that includes calcineurin inhibitors, mycophenolate mofetil, and stroids
medicine
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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
medicine
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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
medicine
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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
medicine
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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
medicine
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a poorer response to mycophenolic acid therapy in some individuals may be due to the presence of the rs11706052 polymorphism
medicine
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IMPDH activity in erythrocytes may be useful indicator of short-term immunosuppression and long-term exposure of the immunosuppressant mycophenolic acid
medicine
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inhibition of IMPDH may represent a novel strategy to reduce adipose tissue mass
medicine
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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
medicine
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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
medicine
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MPDH inhibitors are used as immunosuppressive, antiviral, and anticancer agents
medicine
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MPDH inhibitors are used as immunosuppressive, antiviral, and anticancer agents
medicine
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MPDH inhibitors are used as immunosuppressive, antiviral, and anticancer agents
medicine
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MPDH inhibitors are used as immunosuppressive, antiviral, and anticancer agents